Month: February 2023

Synthesis and evaluation of 2-(2,6-dihalophenyl)-3-pyrimidinyl-1,3-thiazolidin-4-one analogues as anti-HIV-1 agents was written by Rawal, Ravindra K.;Tripathi, Rajkamal;Katti, S. B.;Pannecouque, Christophe;De Clercq, Erik. And the article was included in Bioorganic & Medicinal Chemistry in 2007.Application In Synthesis of 4,6-Diphenylpyrimidin-2-amine This article mentions the following:

A series of 2-(2,6-dihalophenyl)-3-(substituted pyrimidinyl)-1,3-thiazolidin-4-ones were designed on the prediction of quant. structure-activity relationship (QSAR) studies, synthesized, and evaluated as HIV-1 reverse transcriptase inhibitors. Our attempts in correlating the identified mol. surface features related properties for modeling the HIV-1 RT inhibitory activity resulted in some statistically significant QSAR models with good predictive ability. The results showed that compounds 4m (I, R₁ = Cl) and 4n (I, R₁ = F) were highly active in inhibiting HIV-1 replication with EC₅₀ values in the range of 22-28 nM in MT-4 as well as in CEM cells with selectivity indexes of >10,000. The derived models collectively suggest that the compounds should be compact without bulky substitution on its peripheries for better HIV-1 RT inhibitory activity. These models also indicate a preference for hydrophobic compounds to obtain good HIV-1 RT inhibitory activity. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Application In Synthesis of 4,6-Diphenylpyrimidin-2-amine).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. A Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones enables an efficient and facile synthesis of structurally important pyrimidines via a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization.Application In Synthesis of 4,6-Diphenylpyrimidin-2-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery of 3-Oxabicyclo[4.1.0]heptane, a Non-nitrogen Containing Morpholine Isostere, and Its Application in Novel Inhibitors of the PI3K-AKT-mTOR Pathway was written by Hobbs, Heather;Bravi, Gianpaolo;Campbell, Ian;Convery, Maire;Davies, Hannah;Inglis, Graham;Pal, Sandeep;Peace, Simon;Redmond, Joanna;Summers, Declan. And the article was included in Journal of Medicinal Chemistry in 2019.Reference of 62968-37-0 This article mentions the following:

4-(Pyrimidin-4-yl)morpholines are privileged pharmacophores for PI3K and PIKKs inhibition by virtue of the morpholine oxygen, both forming the key hydrogen bonding interaction and conveying selectivity over the broader kinome. Key to the morpholine utility as a kinase hinge binder is its ability to adopt a coplanar conformation with an adjacent aromatic core favored by the morpholine nitrogen nonbonding pair of electrons interacting with the electron deficient pyrimidine π-system. Few selective morpholine replacements have been identified to date. Herein we describe the discovery of a potent non-nitrogen containing morpholine isostere with the ability to mimic this conformation and its application in a potent selective dual inhibitor of mTORC1 and mTORC2 (29b). In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Reference of 62968-37-0).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Reference of 62968-37-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis of 4-amino substituted quinolines and their β-hematin inhibitory activity was written by Singh, Jaybir;Dhakarey, R. K. S.;Singh, Shiv Vardan;Suthar, Manish K.;Saxena, J. K.;Dwivedi, Anil Kumar. And the article was included in Chemistry & Biology Interface in 2012.Related Products of 62968-37-0 This article mentions the following:

In present study, new side chain modified 4-aminoquinoline derivatives and quinoline pyrimidine hybrids were synthesized and evaluated in vitro against β-hematin formation. Compounds 20, 21, 22, 23 have shown significant inhibitory activity against β-hematin formation. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Related Products of 62968-37-0).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Related Products of 62968-37-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis and Antimicrobial Activity of Azolyl Pyrimidines was written by Butta, Ragavendra;Donthamsetty V, Sowmya;Adivireddy, Padmaja;Venkatapuram, Padmavathi. And the article was included in Journal of Heterocyclic Chemistry in 2017.Quality Control of 4,6-Diphenylpyrimidin-2-amine This article mentions the following:

A new class of azolyl pyrimidines I (X = O, S, NH; R = C₆H₅, 4-H₃CC₆H₄, 4-ClC₆H₄, 4-BrC₆H₄, 4-O₂NC₆H₄) linked by diamino sulfone moiety was prepared and their antimicrobial activity was studied. Chloro-substituted and nitro-substituted thiazolyl pyrimidines I (X = S; R = 4-ClC₆H₄ and 4-O₂NC₆H₄) showed excellent antibacterial activity against Bacillus subtilis, while imidazolyl pyrimidines I (X = NH; R = 4-ClC₆H₄ and 4-O₂NC₆H₄) exhibited promising antifungal activity against Aspergillus niger. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Quality Control of 4,6-Diphenylpyrimidin-2-amine).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Quality Control of 4,6-Diphenylpyrimidin-2-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidino piperazinyl acetamides: innovative class of hybrid acetamide drugs as potent antimicrobial and antimycobacterial agents was written by Kanagarajan, V.;Gopalakrishnan, M.. And the article was included in Pharmaceutical Chemistry Journal in 2012.Computed Properties of C16H13N3 This article mentions the following:

New 2-(4-methylpiperazin-1-yl)-N-(4,6-diarylpyrimidin-2-yl)acetamides (34-42) have been synthesized and tested for their in vitro antimicrobial and antimycobacterial properties. Compounds 34, 39 against S. aureus, 39 against β-hemolytic Streptococcus, 42 against V. cholerae, 40-42 against E. coli, 38, 39 against K. pneumoniae, and 37-41 against P. aeruginosa showed excellent antibacterial activity by inhibiting the growth of the resp. organisms at a min. inhibitory concentration of 6.25 μg/mL. Noteworthy compounds 40 against A. flavus, 34 against M. indicus, 40, 42 against R. arrhizus and M. gypseum also exhibited excellent antifungal activity by inhibiting the growth of these microorganisms, at a min. inhibitory concentration of 6.25 μg/mL. Moreover, compounds 36, 38, and 40-42 showed promising antitubercular activity by inhibiting the growth of M. tuberculosis H 37 Rv and clin. isolated isoniazid-resistant M. tuberculosis strains. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Computed Properties of C16H13N3).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Computed Properties of C16H13N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis and characterization of new trifluoromethyl substituted 3-ethoxycarbonyl- and 3-pyrimidin-2-yl-(1,2,3)-oxathiazinane-S-oxides was written by Zanatta, Nilo;Borchhardt, Deise M.;Flores, Darlene C.;Coelho, Helena S.;Marchi, Tiago M.;Flores, Alex F. C.;Bonacorso, Helio G.;Martins, Marcos A. P.. And the article was included in Journal of Heterocyclic Chemistry in 2008.Related Products of 40230-24-8 This article mentions the following:

This paper describes the synthesis and characterization of a new series of 4-substituted 3-ethoxycarbonyl- and 3-(4,6-diphenylpyrimidin-2-yl)-6-trifluoromethyl-(1,2,3)oxathiazinane S-oxides by cyclization of 4,4,4-trifluoro-3-hydroxybutylcarbamates and 4-(4,6-diphenylpyrimidin-2-ylamino)-1,1,1-trifluorobutan-2-ols, resp., with SOCl₂. The anal. of the NMR data allowed us to define important features of the mol. structure. Significant chem. and structural differences were observed between the trifluoromethylated oxathiazinanes obtained in this work from other analogous compounds reported in the literature. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Related Products of 40230-24-8).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Related Products of 40230-24-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Antibiotics in mariculture organisms of different growth stages: Tissue-specific bioaccumulation and influencing factors was written by Zhang, Xuanrui;Zhang, Jiachao;Han, Qianfan;Wang, Xiaoli;Wang, Shuguang;Yuan, Xianzheng;Zhang, Baiyu;Zhao, Shan. And the article was included in Environmental Pollution (Oxford, United Kingdom) in 2021.Name: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide This article mentions the following:

Maricultured organisms are chronically exposed to water containing antibiotics but the bioaccumulative behavior of antibiotics in exposed organisms at different growth stages has received little attention. Here, we investigated the concentrations and tissue-specific bioaccumulation characteristics of 19 antibiotics during three growth stages (youth stage, growth stage, and adult stage) of various organisms (Scophthalmus maximus, Penaeus vannamei, Penaeus japonicus, and Apostichopus japonicus) cultivated in typical marine aquaculture regions, and explored the factors that could affect the bioaccumulation of antibiotics. Tetracyclines (TCs) and fluoroquinolones (FQs) were the dominant antibiotics in all organisms, and the total concentrations of the target antibiotics in fish (S. maximus) were significantly higher than those in shrimp (P. vannamei and P. japonicus) and sea cucumber (A. japonicus) (p < 0.01). The bioaccumulation capacity of a class of statistically significant antibiotics in most samples was strongest during the youth stage and weakest during the adult stage. The antibiotics exhibited higher bioaccumulation capacity in lipid-rich tissues (fish liver and shrimp head) or respiratory organs (fish gill) than muscle. Our results also reveal significant metabolic transformation of enrofloxacin in fish. Different from previous studies, the logarithm bioaccumulation factor (log BAF) was pos. correlated with log Dlipw in low-biotransformation tissues (fish gill and muscle) rather than lipid-rich tissues (fish liver). Based on the calculated hazard quotients (HQ), doxycycline in fish muscle may pose a distinct risk to human health, which deserves special attention. Overall, these results provide insight into the bioaccumulation patterns of antibiotics during different growth stages and tissues of maricultured organisms. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Name: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Name: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis of novel pyrimido[4,5-b]quinolin-4-ones with potential antitumor activity was written by Insuasty, Braulio;Becerra, Diana;Quiroga, Jairo;Abonia, Rodrigo;Nogueras, Manuel;Cobo, Justo. And the article was included in Journal of Heterocyclic Chemistry in 2013.Recommanded Product: 54030-56-7 This article mentions the following:

5,6,7,8,9,10-Hexahydro-2-(methylthio)pyrimido[4,5-b]quinolines and their oxidized forms, the corresponding 6,7,8,9-tetrahydropyrimido[4,5-b]quinolin-4(3H)-ones, were obtained from the reaction of 6-amino-2-(methylthio)pyrimidin-4(3H)-one or its 3-Me derivative and α,β-unsaturated ketones using BF₃.OEt₂ as catalyst and 4-chloranil as oxidizing agent. Some of the new compounds were evaluated in the US National Cancer Institute (NCI), where (9E)-9-benzylidene-3-methyl-2-(methylthio)-5-phenyl-5,6,7,8,9,10-hexahydropyrimido[4,5-b]quinolin-4(3H)-one presented remarkable activity against cancer cell lines, with the most important GI₅₀ values of 0.72-18.4 μM from in vitro assays. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Recommanded Product: 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Recommanded Product: 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine reactions. XXIV. Dehalogenation of 2-halopyrimidines by hydriodic acid was written by Brown, D. J.;Waring, P.. And the article was included in Australian Journal of Chemistry in 1973.Computed Properties of C16H13N3 This article mentions the following:

2-Halopyrimidines underwent dehalogenation conveniently on treatment with hot HI to give the pyrimidines (I; R1 = H, R = R2 = Me, Ph; R = R2 = H, R1 = Me; R1 = R2 = H, R = Me). Unsubstituted pyrimidine was obtained similarly from its 2-chloro-, 2-bromo, or 2-iodo derivative, the last was made in a pure state for the first time. 4-Chloro-2,6-dimethylpyrimidine underwent hydrolysis in hot HI, and transhalogenation to give its 4-iodo analog at lower temperatures; both 2-chloro-4-methoxypyrimidine and 5-chlorouracil gave uracil with hot HI and 4-chloro-2,6-dimethoxypyrimidine gave 6-iodouracil under similar conditions. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Computed Properties of C16H13N3).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. A Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones enables an efficient and facile synthesis of structurally important pyrimidines via a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization.Computed Properties of C16H13N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Oxalic acid catalysed chromium(VI) oxidation of some 2-amino-4,6-diarylpyrimidines was written by Meenakshisundaram, S. P.;Gopalakrishnan, M.;Nagarajan, S.;Sarathi, N.. And the article was included in Catalysis Communications in 2007.SDS of cas: 40230-24-8 This article mentions the following:

Some 2-amino-4,6-diarylpyrimidines (APM), synthesized from chalcones and guanidine hydrochloride in presence of alkali by microwave irradiation in solvent-free conditions, were subjected to oxidation with chromium(VI)-oxalic acid complex (Cr(VI)-Oxa) in highly acidic solutions Oxalic acid (Oxa) offers the reaction a more favorable pathway and in the absence of oxalic acid the reaction is sluggish. The depletion of chromium(VI) shows a complicated kinetics involving a fast reaction to about 35% consumption followed by a slow one. Low dielec. constant of the medium facilitates the reaction. The investigations with 2-amino-6-(4-nitrophenyl)- 4-phenylpyrimidine and 2-amino-6-(4-methoxyphenyl)-4-phenylpyrimidine reveal that, irresp. of the nature of the substituents, the rates are higher than for the parent. APM is catalytically converted to the unusual product 3-hydroxy-1,3-diphenyl-propan-1-one. Consideration of the kinetic behaviors under different exptl. conditions and the product assignment provide valuable mechanistic insight into the system studied. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8SDS of cas: 40230-24-8).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.SDS of cas: 40230-24-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia