Month: October 2022

Pyrimidine is a nitrogenous base similar to benzene (a six-membered ring) and includes cytosine, thymine, and uracil as bases used for DNA or RNA. 109-12-6, formula is C4H5N3, Name is Pyrimidin-2-amine. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Formula: C4H5N3.

Kokkaliari, Sofia;Pham, Kim;Shahbazi, Nargess;Calcul, Laurent;Wojtas, Lukasz;Wilson, Nerida G.;Crawford, Alexander D.;Baker, Bill J. research published 《 Australindolones, New Aminopyrimidine Substituted Indolone Alkaloids from an Antarctic Tunicate Synoicum sp.》, the research content is summarized as follows. Five new alkaloids have been isolated from the lipophilic extract of the Antarctic tunicate Synoicum sp. Deep-sea specimens of Synoicum sp were collected during a 2011 cruise of the R/V Nathanial B. Palmer to the southern Scotia Arc, Antarctica. Crude extracts from the invertebrates obtained during the cruise were screened in a zebrafish-based phenotypic assay. The Synoicum sp extract induced embryonic dysmorphol. characterized by axis truncation, leading to the isolation of aminopyrimidine substituted indolone (1-4) and indole (5-12) alkaloids. While the primary bioactivity tracked with previously reported meridianins A-G (5-11), further investigation resulted in the isolation and characterization of australindolones A-D (1-4) and the previously unreported meridianin H (12).

Formula: C4H5N3, 2-Aminopyrimidine is a useful research compound. Its molecular formula is C4H5N3 and its molecular weight is 95.1 g/mol. The purity is usually 95%.
2-Aminopyrimidine is an organic compound that belongs to the group of pyridines. It has been shown to have antimicrobial, antitumor, and antiviral properties. 2-Aminopyrimidine has been used as a fungicide and herbicide in horticulture and agriculture, respectively. The molecular geometry of this molecule is octahedral with coordination geometry C2v. This chemical binds to the BCR-ABL kinase receptor and inhibits its activity by competitive inhibition of ATP binding. 2-Aminopyrimidine has been shown to have a hematologic response in vivo models and in vitro assays. It also has anti-inflammatory effects when it is taken orally or applied topically., 109-12-6.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 65-86-1, formula is C5H4N2O4, Name is 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Computed Properties of 65-86-1.

Kneller, Daniel W.;Li, Hui;Galanie, Stephanie;Phillips, Gwyndalyn;Labbe, Audrey;Weiss, Kevin L.;Zhang, Qiu;Arnould, Mark A.;Clyde, Austin;Ma, Heng;Ramanathan, Arvind;Jonsson, Colleen B.;Head, Martha S.;Coates, Leighton;Louis, John M.;Bonnesen, Peter V.;Kovalevsky, Andrey research published 《 Structural, electronic, and electrostatic determinants for inhibitor binding to subsites S1 and S2 in SARS-CoV-2 main protease》, the research content is summarized as follows. Creating small-mol. antivirals specific for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) proteins is crucial to battle coronavirus disease 2019 (COVID-19). SARS-CoV-2 main protease (M^pro) is an established drug target for the design of protease inhibitors. We performed a structure-activity relationship (SAR) study of noncovalent compounds that bind in the enzyme’s substrate-binding subsites S1 and S2, revealing structural, electronic, and electrostatic determinants of these sites. The study was guided by the X-ray/neutron structure of M^pro complexed with Mcule-5948770040 (I), in which protonation states were directly visualized. Virtual reality-assisted structure anal. and small-mol. building were employed to generate analogs of I. In vitro enzyme inhibition assays and room-temperature X-ray structures demonstrated the effect of chem. modifications on M^pro inhibition, showing that (1) maintaining correct geometry of an inhibitor’s P1 group is essential to preserve the hydrogen bond with the protonated His163; (2) a pos. charged linker is preferred; and (3) subsite S2 prefers nonbulky modestly electroneg. groups.

Computed Properties of 65-86-1, Orotic acid anhydrous is a hydrogen bonding interaction that can be found in biological systems. It plays a role in the physiological effects of orotic acid, which is a metabolite of uridine and an intermediate in the synthesis of pyrimidine nucleotides. Orotic acid has antimicrobial properties and has been shown to inhibit enzyme activities involved in energy metabolism, such as polymerase chain reaction (PCR) and adenosine triphosphate (ATP) synthase. Orotic acid also inhibits the growth of bacteria, fungi, and parasites. Orotic acid anhydrous is used for treating myocardial infarcts or brain functions. The untreated group was given no treatment at all.
Orotic acid, also known as orotate or orotsaeure, belongs to the class of organic compounds known as pyrimidinecarboxylic acids. These are pyrimidines with a structure containing a carboxyl group attached to the pyrimidine ring. Orotic acid exists as a solid, slightly soluble (in water), and a moderately acidic compound (based on its pKa). Orotic acid has been found in human liver and pancreas tissues, and has also been primarily detected in saliva, feces, urine, and blood. Within the cell, orotic acid is primarily located in the cytoplasm and mitochondria. Orotic acid exists in all eukaryotes, ranging from yeast to humans. Orotic acid participates in a number of enzymatic reactions. In particular, Orotic acid can be biosynthesized from L-dihydroorotic acid and quinone; which is mediated by the enzyme dihydroorotate dehydrogenase (quinone), mitochondrial. In addition, Orotic acid and phosphoribosyl pyrophosphate can be converted into orotidylic acid through its interaction with the enzyme uridine monophosphate synthetase isoform a. In humans, orotic acid is involved in the pyrimidine metabolism pathway. Orotic acid is also involved in several metabolic disorders, some of which include the mngie (mitochondrial neurogastrointestinal encephalopathy) pathway, dihydropyrimidinase deficiency, UMP synthase deficiency (orotic aciduria), and Beta ureidopropionase deficiency. Outside of the human body, orotic acid can be found in a number of food items such as green vegetables, alaska blueberry, chickpea, and colorado pinyon. This makes orotic acid a potential biomarker for the consumption of these food products. Orotic acid is a potentially toxic compound. Orotic acid has been found to be associated with several diseases known as phosphoenolpyruvate carboxykinase deficiency 1, cytosolic and hyperornithinemia-hyperammonemia-homocitrullinuria; orotic acid has also been linked to several inborn metabolic disorders including n-acetylglutamate synthetase deficiency, lysinuric protein intolerance, and ornithine transcarbamylase deficiency.
Orotic acid appears as white crystals or crystalline powder.
Orotic acid is a pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6. It has a role as a metabolite, an Escherichia coli metabolite and a mouse metabolite. It derives from a uracil. It is a conjugate acid of an orotate., 65-86-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 4595-59-9, formula is C4H3BrN2, Name is 5-Bromopyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Application of C4H3BrN2.

Kloevekorn, Philip;Pfaffenrot, Bent;Juchum, Michael;Selig, Roland;Albrecht, Wolfgang;Zender, Lars;Laufer, Stefan A. research published 《 From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4)》, the research content is summarized as follows. The mitogen-activated protein kinase (MAP) kinase 4 (MKK4) was found to be a major regulator of liver regeneration and could be a valuable drug target addressing liver related diseases by restoring its intrinsic regenerative capacity. We report on the synthesis and optimization of novel MKK4 inhibitors following a target-hopping strategy from the FDA-approved BRAF^V600E inhibitor PLX4032 (8, I). Applying an iterative multi-parameter optimization process we carved out essential structural features yielding in compounds with a low nanomolar affinity for MKK4 and excellent selectivity profiles against the main off-targets MKK7 and JNK1, which, upon relevant inhibition, would totally abrogate the pro-regenerative effect of MKK4 inhibition, as well as against the off-targets MAP4K5, ZAK and BRAF with selectivity factors ranging from 40 to 430 for our best-balanced compounds 70 and 73 (II and III, resp.).

4595-59-9, 5-Bromopyrimidine is a reactive intermediate that is used in the synthesis of 4-methoxyphenylboronic acid. 5-Bromopyrimidine has been shown to be nucleophilic, reacting with β-amino acids under basic conditions to form the corresponding 2-bromo amide. It also undergoes cross-coupling reactions with halides and can be used as a building block for other organic compounds. 5-Bromopyrimidine has optical properties that are characteristic of aromatic molecules, including strong absorption bands in the ultraviolet region and visible light region.
5-Bromopyrimidine undergoes direct metallation with lithuium diisopropylamide to yield 4-lithio-5-bromopyrimidine., Application of C4H3BrN2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The nomenclature of pyrimidines is straightforward. However, like other heterocyclics, tautomeric hydroxyl groups yield complications since they exist primarily in the cyclic amide form. 4595-59-9, formula is C4H3BrN2, Name is 5-Bromopyrimidine. For example, 2-hydroxypyrimidine is more properly named 2-pyrimidone. A partial list of trivial names of various pyrimidines exists. Safety of 5-Bromopyrimidine.

Klikar, Milan;Georgiou, Dimitris;Polyzos, Ioannis;Fakis, Mihalis;Ruzickova, Zdenka;Pytela, Oldrich;Bures, Filip research published 《 Triphenylamine-based fluorophores bearing peripheral diazine regioisomers. Synthesis, characterization, photophysics and two-photon absorption》, the research content is summarized as follows. Six tripodal push-pull fluorophores with D-(π-A₃) arrangement were designed and synthesized. The structure of these fluorophores consists of a central electron-donating triphenylamine core and peripheral electron-withdrawing diazine units (pyridazine, pyrimidine, and pyrazine moieties), which are linked by an ethynylene π-spacer. The preparation of the fluorophores involves 3-fold Sonogashira cross-coupling reaction starting from the key tris(4-ethynylphenyl)amine intermediate. The structure and spatial arrangement of 2 fluorophores were completely confirmed by x-ray anal. Thermal and electrochem. behavior of prepared fluorophores were studied by DSC and cyclic voltammetry. Their linear optical properties were examined by UV-visible absorption, steady-state and time resolved fluorescent spectroscopy while 2 PA anal. was used for a study of the nonlinear optical response. Exptl. data were supported by DFT calculations Based on the exptl. as well as theor. data, structure-property relations were thoroughly revealed.

4595-59-9, 5-Bromopyrimidine is a reactive intermediate that is used in the synthesis of 4-methoxyphenylboronic acid. 5-Bromopyrimidine has been shown to be nucleophilic, reacting with β-amino acids under basic conditions to form the corresponding 2-bromo amide. It also undergoes cross-coupling reactions with halides and can be used as a building block for other organic compounds. 5-Bromopyrimidine has optical properties that are characteristic of aromatic molecules, including strong absorption bands in the ultraviolet region and visible light region.
5-Bromopyrimidine undergoes direct metallation with lithuium diisopropylamide to yield 4-lithio-5-bromopyrimidine., Safety of 5-Bromopyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 4595-59-9, formula is C4H3BrN2, Name is 5-Bromopyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Quality Control of 4595-59-9.

Kim, Weonjeong;Koo, Jangwoo;Lee, Hong Geun research published 《 Benzylic C(sp³)-C(sp²) cross-coupling of indoles enabled by oxidative radical generation and nickel catalysis》, the research content is summarized as follows. A mechanistically unique functionalization strategy for a benzylic C(sp³)-H bond was developed based on facile oxidation event of indole substrates. This novel pathway was initiated by efficient radical generation at benzylic position of substrate, with subsequent transition metal catalysis to complete overall transformation. Ultimately, an aryl or an acyl group could be effectively delivered from an aryl (pseudo)halide or an acid anhydride coupling partner, resp. The developed method utilized mild conditions and exhibited a wide substrate scope for both substituted indoles and C(sp²)-based reaction counterparts. Mechanistic studies showed that competitive hydrogen atom transfer (HAT) processes, which were frequently encountered in conventional methods, are not involved in the product formation process of the developed strategy.

4595-59-9, 5-Bromopyrimidine is a reactive intermediate that is used in the synthesis of 4-methoxyphenylboronic acid. 5-Bromopyrimidine has been shown to be nucleophilic, reacting with β-amino acids under basic conditions to form the corresponding 2-bromo amide. It also undergoes cross-coupling reactions with halides and can be used as a building block for other organic compounds. 5-Bromopyrimidine has optical properties that are characteristic of aromatic molecules, including strong absorption bands in the ultraviolet region and visible light region.
5-Bromopyrimidine undergoes direct metallation with lithuium diisopropylamide to yield 4-lithio-5-bromopyrimidine., Quality Control of 4595-59-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Safety of 2,4-Dichloro-5-fluoropyrimidine.

Kim, Juhyeon;Kim, Yoon Jung;Londhe, Ashwini M.;Pae, Ae Nim;Choo, Hyunah;Kim, Hak Joong;Min, Sun-Joon research published 《 Synthesis and biological evaluation of disubstituted pyrimidines as selective 5-HT2C agonists》, the research content is summarized as follows. The synthesis of disubstituted pyrimidine derivatives I [R¹ = 3-F, 4-F; n = 0, 1, 2; R² = piperazin-1-yl, (2R)-2-methylpiperazin-1-yl, 1,4-diazepan-1-yl], II [R³ = (2R)-2-(3-fluorophenyl)propyl, (2R)-2-(4-fluorophenyl)propyl, 3-fluorophenyl, 4-fluorophenyl; R⁴ = 1,4-diazepan-1-yl, [(3R)-pyrrolidin-3-yl]aminyl, 2,7-diazaspiro[4.4]nonan-2-yl, etc.] and their biol. evaluation as selective 5-HT2C agonists were described. To improve selectivity for 5-HT2C over other subtypes, two series of disubstituted pyrimidines with fluorophenylalkoxy groups at either the 5-position or 4-position and varying cyclic amines at the 2-position were synthesized. The in vitro cell-based assay and binding assay identified compounds II [R³ = (2R)-2-(3-fluorophenyl)propyl, R⁴ = 1,4-diazepan-1-yl (I); R³ = (2R)-2-(4-fluorophenyl)propyl, R⁴ = 1,4-diazepan-1-yl] as potent 5-HT2C agonists. Further studies on selectivity to 5-HT subtypes and drug-like properties indicated that 2,4-disubstituted pyrimidine (I) showed a highly agonistic effect on the 5-HT2C receptor, with excellent selectivity, as well as exceptional drug-like properties, including high plasma and microsomal stability, along with low CYP inhibition. Thus, pyrimidine (I) could be considered a viable lead compound as a 5-HT2C selective agonist.

Safety of 2,4-Dichloro-5-fluoropyrimidine, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The nomenclature of pyrimidines is straightforward. However, like other heterocyclics, tautomeric hydroxyl groups yield complications since they exist primarily in the cyclic amide form. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. For example, 2-hydroxypyrimidine is more properly named 2-pyrimidone. A partial list of trivial names of various pyrimidines exists. Formula: C4HCl2FN2.

Kim, Juhyeon;Jo, Hanbyeol;Lee, Hyunseung;Choo, Hyunah;Kim, Hak Joong;Pae, Ae Nim;Cho, Yong Seo;Min, Sun-Joon research published 《 Identification of optically active pyrimidine derivatives as selective 5-HT_2C modulators》, the research content is summarized as follows. A series of pyrimidine derivatives I [R = 2-F, 3-F, 4-F; R¹ = H, Me; n = 0, 2] was synthesized and evaluated for their binding affinities toward 5-HT_2C receptors. With regard to designed mols. I, the influence of size of alkyl ether and the absolute configuration of a stereogenic center on the 5-HT_2C binding affinity and selectivity was studied. The most promising diastereomeric mixtures I [R = 3-F, 4-F; R¹ = Me; n = 0] were selected in the initial radioligand binding assay and they were further synthesized as optically active forms starting from optically active alcs. RC₆H₄CH₂CH(Me)OH [stereo – R or S] by enzymic kinetic resolution Pyrimidine analog I [R = 4-F, R¹ = Me, n = 0, stereo – (R,R)] displayed an excellent 5-HT_2C binding affinity with good selectivity values against a broad range of other 5-HT receptor subtypes.

Formula: C4HCl2FN2, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Reference of 2927-71-1.

Kim, Juhyeon;Moon, Byung Seok;Lee, Byung Chul;Lee, Ho-Young;Kim, Hak-Joong;Choo, Hyunah;Pae, Ae Nim;Cho, Yong Seo;Min, Sun-Joon research published 《 A Potential PET Radiotracer for the 5-HT_2C Receptor: Synthesis and in Vivo Evaluation of 4-(3-[¹⁸F]fluorophenethoxy)pyrimidine》, the research content is summarized as follows. The serotonin 2C receptor subtype (5-HT2C) is an excitatory 5-HT receptor widely distributed throughout the central nerve system. As the 5-HT2C receptor displays multiple actions on various neurotransmitter systems including glutamate, dopamine, epinephrine and γ-aminobutyric acid (GABA), abnormalities of the 5-HT2C receptor are associated with psychiatric diseases such as depression, schizophrenia, drug abuse, and anxiety. Up to date, three kinds of 5-HT2C PET radiotracers such as [11C]N-methylated arylazepine (1), [11C]WAY-163909 (2), [18F]fluorophenylcyclopropane (3) have been developed, but they may not be suitable for in vivo 5-HT2C imaging study due to their modest specific binding. Herein, the synthesis and in vivo evaluation of 4-(3-[18F]fluorophenethoxy)pyrimidine [18F]4 as a potential PET radiotracer for the 5-HT2C receptor is described. [18F]4 was synthesized by nucleophilic aromatic substitution of diaryliodonium precursor 17a with a 7.8 ± 2.7% (n = 6, decay corrected) radiochem. yield and over 99% radiochem. purity, showing an 89 ± 14 GBq/μmol specific radioactivity. The in vivo PET imaging studies of [18F]4 with or without locaserin, an FDA approved selective 5-HT2C agonist, demonstrated that [18F]4 exhibits a high level of specific binding to 5-HT2C receptors in the rat brain.

Reference of 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. 65-86-1, formula is C5H4N2O4, Name is 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid. It is also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Quality Control of 65-86-1.

Kim, Hyung Joon;Kim, Ju Hyun;Yeon, Jong Eun;Seo, Yeon Seok;Jang, Jeong Won;Cho, Yong Kyun;Jang, Byoung Kuk;Han, Byung Hoon;Lee, Changhyeong;Lee, Joon Hyeok;Yoon, Jung-Hwan;Kim, Kang Mo;Kim, Moon Young;Kim, Do Young;Park, Neung Hwa;Cho, Eun Young;Lee, June Sung;Lee, Jin-Woo;Kim, In Hee;Song, Byung-Cheol;Lee, Byung-Seok;Kwon, Oh Sang research published 《 A multi-center, double-blind randomized controlled phase III clinical trial to evaluate the antiviral activity and safety of DA-2802 (tenofovir disoproxil orotate) and viread (tenofovir disoproxil fumarate) in chronic hepatitis b patients》, the research content is summarized as follows. Background: Tenofovir disoproxil fumarate (TDF, Viread) had been used as a standard treatment option of chronic hepatitis B (CHB). This clin. trial was conducted to evaluate the efficacy and safety of DA-2802 (tenofovir disoproxil orotate) compared to TDF. Methods: The present study was a double blind randomized controlled trial. Patients with CHB were recruited from 25 hospitals in Korea and given DA-2802 at a dose of 319 mg once daily or Viread at a dose of 300 mg once daily for 48 wk from March 2017 to Jan. 2019. Change in hepatitis B virus (HBV) DNA level at week 48 after dosing compared to baseline was the primary efficacy endpoint. Secondary efficacy endpoints were proportions of subjects with undetectable HBV DNA, those with normal alanine aminotransferase (ALT) levels, and those with loss of hepatitis B envelop antigen (HBeAg), those with loss of hepatitis B surface antigen (HBsAg). Adverse events (AEs) were also investigated. Results: A total of 122 patients (DA-2802 group: n = 61, Viread group: n = 61) were used as full anal. set for efficacy anal. Mean age, proportion of males, laboratory results and virol. characteristics were not different between the two groups. The change in HBV DNA level at week 48 from baseline was -5.13 ± 1.40 in the DA-2802 group and -4.97 ± 1.40 log10 copies/mL in the Viread group. The anal. of primary endpoint using the nonparametric anal. of covariance showed statistically significant results (P < 0.001), which confirmed non-inferiority of DA-2802 to Viread by a prespecified noninferiority margin of 1. The proportion of undetectable HBV DNA was 78.7% in the DA-2802 group and 75.4% in the Viread group (P = 0.698). The proportion of subjects who had normal ALT levels was 75.4% in the DA-2802 group and 73.3% in the Viread group (P = 0.795). The proportion of those with HBeAg loss was 8.1% in the DA-2802 group and 10.8% in the Viread group (P = 1.000). No subject showed HBsAg loss. The frequency of AEs during treatment was similar between the two groups. Most AEs were mild to moderate in severity. Conclusion: DA-2802 is considered an effective and safe treatment for patients with CHB.

Quality Control of 65-86-1, Orotic acid anhydrous is a hydrogen bonding interaction that can be found in biological systems. It plays a role in the physiological effects of orotic acid, which is a metabolite of uridine and an intermediate in the synthesis of pyrimidine nucleotides. Orotic acid has antimicrobial properties and has been shown to inhibit enzyme activities involved in energy metabolism, such as polymerase chain reaction (PCR) and adenosine triphosphate (ATP) synthase. Orotic acid also inhibits the growth of bacteria, fungi, and parasites. Orotic acid anhydrous is used for treating myocardial infarcts or brain functions. The untreated group was given no treatment at all.
Orotic acid, also known as orotate or orotsaeure, belongs to the class of organic compounds known as pyrimidinecarboxylic acids. These are pyrimidines with a structure containing a carboxyl group attached to the pyrimidine ring. Orotic acid exists as a solid, slightly soluble (in water), and a moderately acidic compound (based on its pKa). Orotic acid has been found in human liver and pancreas tissues, and has also been primarily detected in saliva, feces, urine, and blood. Within the cell, orotic acid is primarily located in the cytoplasm and mitochondria. Orotic acid exists in all eukaryotes, ranging from yeast to humans. Orotic acid participates in a number of enzymatic reactions. In particular, Orotic acid can be biosynthesized from L-dihydroorotic acid and quinone; which is mediated by the enzyme dihydroorotate dehydrogenase (quinone), mitochondrial. In addition, Orotic acid and phosphoribosyl pyrophosphate can be converted into orotidylic acid through its interaction with the enzyme uridine monophosphate synthetase isoform a. In humans, orotic acid is involved in the pyrimidine metabolism pathway. Orotic acid is also involved in several metabolic disorders, some of which include the mngie (mitochondrial neurogastrointestinal encephalopathy) pathway, dihydropyrimidinase deficiency, UMP synthase deficiency (orotic aciduria), and Beta ureidopropionase deficiency. Outside of the human body, orotic acid can be found in a number of food items such as green vegetables, alaska blueberry, chickpea, and colorado pinyon. This makes orotic acid a potential biomarker for the consumption of these food products. Orotic acid is a potentially toxic compound. Orotic acid has been found to be associated with several diseases known as phosphoenolpyruvate carboxykinase deficiency 1, cytosolic and hyperornithinemia-hyperammonemia-homocitrullinuria; orotic acid has also been linked to several inborn metabolic disorders including n-acetylglutamate synthetase deficiency, lysinuric protein intolerance, and ornithine transcarbamylase deficiency.
Orotic acid appears as white crystals or crystalline powder.
Orotic acid is a pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6. It has a role as a metabolite, an Escherichia coli metabolite and a mouse metabolite. It derives from a uracil. It is a conjugate acid of an orotate., 65-86-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 65-86-1, formula is C5H4N2O4, Name is 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Safety of 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid.

Kim, Hye-Shin;Arellano, Karina;Park, Haryung;Todorov, Svetoslav D.;Kim, Bobae;Kang, Hyeji;Park, Yu Jin;Suh, Dong Ho;Jung, Eun Sung;Ji, Yosep;Holzapfel, Wilhelm H. research published 《 Assessment of the safety and anti-inflammatory effects of three Bacillus strains in the respiratory tract》, the research content is summarized as follows. Chronic respiratory diseases are part of accumulating health problems partly due to worldwide increase in air pollution. By their antimicrobial and immunomodulatory properties, some probiotics constitute promising alternatives for the prevention and treatment of chronic respiratory diseases. We have isolated Bacillus strains from Korean fermented foods and selected three potentially probiotic strains (two Bacillus subtilis and one Bacillus amyloliquefaciens) based on safety, antimicrobial efficacy, activity against airborne pathogens and their immunomodulatory properties in vivo. Safety evaluation included in silico anal. for confirming absence of virulence genes. Safety for the respiratory tract was confirmed by an in vivo pathogenicity test using a murine model. Antimicrobial activity was displayed against several airborne pathogens. Potential antimicrobial metabolites such as 2,3-butanediol and propylene glycol were identified as possible antagonistic agents. Immunomodulatory properties in vitro were confirmed by upregulation of IL-10 expression in a macrophage cell line. Intranasal instillation and inhalation in an ovalbumin (OVA)-induced lung inflammation murine model reduced T helper type 2 (Th2) cytokines at transcriptional and protein levels in the lungs. The safety and potentially beneficial role of these Bacillus strains could be demonstrated for the respiratory tract of a murine model. The obtained 16S rRNA partial sequences were deposited in the gene bank as accession numbers MW709435 (B. subtilis 3), MW709437(B. subtilis 281), and MW709530 (B. amyloliquefaciens 298).

65-86-1, Orotic acid anhydrous is a hydrogen bonding interaction that can be found in biological systems. It plays a role in the physiological effects of orotic acid, which is a metabolite of uridine and an intermediate in the synthesis of pyrimidine nucleotides. Orotic acid has antimicrobial properties and has been shown to inhibit enzyme activities involved in energy metabolism, such as polymerase chain reaction (PCR) and adenosine triphosphate (ATP) synthase. Orotic acid also inhibits the growth of bacteria, fungi, and parasites. Orotic acid anhydrous is used for treating myocardial infarcts or brain functions. The untreated group was given no treatment at all.
Orotic acid, also known as orotate or orotsaeure, belongs to the class of organic compounds known as pyrimidinecarboxylic acids. These are pyrimidines with a structure containing a carboxyl group attached to the pyrimidine ring. Orotic acid exists as a solid, slightly soluble (in water), and a moderately acidic compound (based on its pKa). Orotic acid has been found in human liver and pancreas tissues, and has also been primarily detected in saliva, feces, urine, and blood. Within the cell, orotic acid is primarily located in the cytoplasm and mitochondria. Orotic acid exists in all eukaryotes, ranging from yeast to humans. Orotic acid participates in a number of enzymatic reactions. In particular, Orotic acid can be biosynthesized from L-dihydroorotic acid and quinone; which is mediated by the enzyme dihydroorotate dehydrogenase (quinone), mitochondrial. In addition, Orotic acid and phosphoribosyl pyrophosphate can be converted into orotidylic acid through its interaction with the enzyme uridine monophosphate synthetase isoform a. In humans, orotic acid is involved in the pyrimidine metabolism pathway. Orotic acid is also involved in several metabolic disorders, some of which include the mngie (mitochondrial neurogastrointestinal encephalopathy) pathway, dihydropyrimidinase deficiency, UMP synthase deficiency (orotic aciduria), and Beta ureidopropionase deficiency. Outside of the human body, orotic acid can be found in a number of food items such as green vegetables, alaska blueberry, chickpea, and colorado pinyon. This makes orotic acid a potential biomarker for the consumption of these food products. Orotic acid is a potentially toxic compound. Orotic acid has been found to be associated with several diseases known as phosphoenolpyruvate carboxykinase deficiency 1, cytosolic and hyperornithinemia-hyperammonemia-homocitrullinuria; orotic acid has also been linked to several inborn metabolic disorders including n-acetylglutamate synthetase deficiency, lysinuric protein intolerance, and ornithine transcarbamylase deficiency.
Orotic acid appears as white crystals or crystalline powder.
Orotic acid is a pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6. It has a role as a metabolite, an Escherichia coli metabolite and a mouse metabolite. It derives from a uracil. It is a conjugate acid of an orotate., Safety of 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia