Tag: 200-300

2,4,6-Trisubstituted pyrimidines as a new class of selective adenosine A₁ receptor antagonists was written by Chang, Lisa C. W.;Spanjersberg, Ronald F.;von Kuenzel, Jacobien K.;Mulder-Krieger, Thea;van den Hout, Gijs;Beukers, Margot W.;Brussee, Johannes;Ijzerman, Adriaan P.. And the article was included in Journal of Medicinal Chemistry in 2004.Recommanded Product: 4,6-Diphenylpyrimidin-2-amine This article mentions the following:

Adenosine receptor antagonists usually possess a bi- or tricyclic heteroaromatic structure at their core with varying substitution patterns to achieve selectivity and/or greater affinity. Taking into account mol. modeling results from a series of potent adenosine A₁ receptor antagonists, a pharmacophore was derived from which a monocyclic core can be equally effective. To achieve a compound that may act at the CNS, a restriction related to its polar surface area (PSA) was proposed. In consequence, two series of pyrimidines, e.g., I, possessing good potency at the adenosine A₁ receptor and desirable PSA values were synthesized. In particular, I (LUF 5735) displayed excellent A₁ affinity (K_i = 4 nM) and selectivity (≤50% displacement of 1 μM concentrations of the radioligand at the other three adenosine receptors) and has a PSA value of 53 Ų. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Recommanded Product: 4,6-Diphenylpyrimidin-2-amine).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. 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.Recommanded Product: 4,6-Diphenylpyrimidin-2-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Occurrence of veterinary antibiotics in animal manure, compost, and agricultural soil, originating from different feedlots in suburbs of Shanghai, East China was written by Qian, Xiaoyong;Wang, Zhenqi;Zhang, Hongchang;Gu, Hairong;Shen, Genxiang. And the article was included in Environmental Monitoring and Assessment in 2022.Reference of 1220-83-3 This article mentions the following:

The present study aims to monitor and assess the occurrence of veterinary antibiotics (VAs) in animal manure, compost, and fertilized soil, originating from different large-scale feedlots. The corresponding concentrations of 39 types of VAs in 8 large-scale feedlots of pig, dairy cow, and poultry were sampled in different seasons and analyzed using LC-MS. The results indicated that 17 types, 16 types, and 5 types of VAs were detected in the swine manure, compost, and fertilized soil with the concentrations of 0.003-17.82, 0.002-9.59, and 0.004-0.007 mg kg-1 (dry matter), resp.; 3 types, 2 types, and 1 type of VAs were detected in the dairy manure, compost, and fertilized soil with the concentrations of 0.003-1.94, 0.014-0.044, and 0.025 mg kg-1 (dry matter), resp.; 7 types, 5 types, and 1 type of VAs were detected in the poultry manure, compost, and fertilized soil with the concentrations of 0.035-1.06, 0.018-0.049, and 0.019 mg kg-1 (dry matter), resp. The main antibiotic classes persisted in the animal manure and their composting product and fertilized soil were sulfonamides (SAs), macrolides (MAs), and tetracyclines (TCs). Thus, this study would help to adopt strategies in pollution control of VAs and environmental protection of agriculture. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Reference of 1220-83-3).

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. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Reference of 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Determination of organic pollutants in water by off-line supercritical fluid extraction-gas chromatography/infrared spectrometry/mass spectrometry was written by Ren, Li;Wang, Guojun. And the article was included in Sepu in 1998.Category: pyrimidines This article mentions the following:

A supercritical fluid extraction (SFE) method using carbon dioxide for the determination of organic pollutants in Yellow River water was developed. In this paper, organic contaminants in 3L Yellow River water were concentrated on 1g GDX-301 adsorbent and then eluted from the adsorbent with supercritical CO₂. The analytes extracted by SFE were collected into 1mL alc. collecting solvent through a SiO₂ restrictor (35cm x 50μm i.d.). Finally, the collecting solvent was analyzed by Gas Chromatog./IR Spectrometry/Mass Spectrometry. The SFE conditions which were optimized for removal of the analytes from adsorbent were 20MPa, 60°C and 40min. The extraction efficiencies of SFE were directly compared to those obtained by using 15mL dichloromethane elution. Efficiencies of SFE under conditions of 20MPa, 60°C and 40min were generally higher than those of solvent elution. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Category: pyrimidines).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. 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.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Response of fungi-microalgae pellets to copper regulation in the removal of sulfonamides and release of dissolved organic matters was written by Li, Shuangxi;Li, Zhuo;Liu, Dongyang;Yin, Zhihong;Hu, Dan;Yu, Yunjiang;Li, Zhaohua;Zhu, Liandong. And the article was included in Journal of Hazardous Materials in 2022.Name: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide This article mentions the following:

Both sulfonamides (SAs) and copper (Cu(II)) were frequently detected together in swine wastewater. In this study, the regulation of Cu(II) on SAs adsorption and release of dissolved organic matters (DOMs) by fungi-microalgae pellets (FM-pellets) were investigated. Aspergillus oryzae pellets were prepared for combination with Chlorella vulgaris and the optimal conditions were at agitation speed of 130 rpm, fungi to microalgae ratio of 10:1 and the combined time of 3 h with the highest combination efficiency of 98.65%. The results showed that adsorption was the main mechanism for SAs removal. FM-pellets exhibited a high SAs adsorption potential within 6 h, and the adsorption capacity of sulfamethazine (SMZ), sulfamonomethoxine (SMM) and sulfamethoxazole (SMX) was 1.07, 0.94 and 1.67 mg/g, resp. Furthermore, the removal of SMX, SMZ and SMM was greatly promoted from 62.31% to 85.21%, 58.71-67.91% and 64.17-80.31%, resp., under the presence of 2 mg/L Cu(II) through ion exchange and adsorption bridging. DOMs were analyzed by the parallel factor (PARAFAC) to demonstrate the response mechanism of FM-pellets to Cu(II). Protein-like substances and NADH in DOMs released by FM-pellets formed complexes with Cu(II) to alleviate the damage on the organism. These findings provide new insights into the mechanism and response of Cu(II) in the removal of SAs by FM-pellets. 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. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Name: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators was written by Chekler, Eugene L. Piatnitski;Unwalla, Rayomond;Khan, Taukeer A.;Tangirala, Raghuram S.;Johnson, Mark;St. Andre, Michael;Anderson, James T.;Kenney, Thomas;Chiparri, Sue;McNally, Chris;Kilbourne, Edward;Thompson, Catherine;Nagpal, Sunil;Weber, Gregory;Schelling, Scott;Owens, Jane;Morris, Carl A.;Powell, Dennis;Verhoest, Patrick R.;Gilbert, Adam M.. And the article was included in Journal of Medicinal Chemistry in 2014.Computed Properties of C7H6Cl2N2O2 This article mentions the following:

We present a novel series of selective androgen receptor modulators (SARMs) which shows excellent biol. activity and phys. properties. 1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)-indoline-4-carbonitriles showed potent binding to the androgen receptor (AR) and activated AR-mediated transcription in vitro. Representative compounds demonstrated diminished activity in promoting the intramol. interaction between the AR carboxyl (C) and amino (N) termini. This N/C-termini interaction is a biomarker assay for the undesired androgenic responses in vivo. In orchidectomized rats, daily administration of a lead compound from this series showed anabolic activity by increasing levator ani muscle weight Importantly, minimal androgenic effects (increased tissue weights) were observed in the prostate and seminal vesicles, along with minimal repression of circulating LH (LH) levels and no change in the lipid and triglyceride levels. This lead compound completed a two week rat toxicol. study, and was well tolerated at doses up to 100 mg/kg/day, the highest dose tested, for 14 consecutive days. In the experiment, the researchers used many compounds, for example, Methyl 2-(4,6-dichloropyrimidin-5-yl)acetate (cas: 171096-33-6Computed Properties of C7H6Cl2N2O2).

Methyl 2-(4,6-dichloropyrimidin-5-yl)acetate (cas: 171096-33-6) 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 C7H6Cl2N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer was written by Wu, Zhengyang;Bai, Ying;Jin, Jiaming;Jiang, Teng;Shen, Hui;Ju, Qiurong;Zhu, Qihua;Xu, Yungen. And the article was included in European Journal of Medicinal Chemistry in 2021.Recommanded Product: 2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine This article mentions the following:

PARP inhibitors have achieved great success in cancers with BRCA mutations, but only a small portion of patients carry BRCA mutations, which results in their narrow indication spectrum. Recently, emerging evidence has demonstrated that combinations of PARP and PI3K inhibitors could evoke unanticipated synergistic effects in various cancers, even including BRCA-proficient ones. In this work, a series of PARP/PI3K dual inhibitors were designed, synthesized, and evaluated for their biol. activities. It was found that compounds 9a and 23a exhibited excellent inhibitory activities against PARP-1 (9a: IC50 = 1.57 nM, 23a: IC50 = 0.91 nM) and PI3Kα (9a: IC50 = 2.0 nM, 23a: IC50 = 1.5 nM), and showed promising antiproliferative activities against both BRCA-deficient (HCT-116, HCC-1937) and BRCA-proficient (SW620, MDA-MB-231/468) tumor cells. 9a and 23a also exhibited considerable in vivo antitumor efficacy in an MDA-MB-468 xenograft mouse model, with TGI values of 56.39% and 48.77%, resp. Addnl., 23a possessed promising profiles including high kinase selectivity and low cardiotoxicity. Overall, this work indicates 9a and 23a might be potential PARP/PI3K dual inhibitors for cancer therapy and deserve further research. In the experiment, the researchers used many compounds, for example, 2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine (cas: 35265-83-9Recommanded Product: 2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine).

2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine (cas: 35265-83-9) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Recommanded Product: 2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Antibiotics biomonitored in urine and obesogenic risk in a community-dwelling elderly population was written by Sang, Yanru;Zhang, Jingjing;Liu, Kaiyong;Wang, Qunan;Wang, Sufang;Sheng, Jie;Wang, Li;Zhang, Dongmei;Li, Xiude;Cao, Hongjuan;Liu, Annuo;Tao, Fangbiao. And the article was included in Ecotoxicology and Environmental Safety in 2021.Electric Literature of C11H12N4O3S This article mentions the following:

Exptl. and epidemiol. studies have linked antibiotics use to gut dysbiosis-mediated risk of chronic metabolic diseases. However, whether adiposity is linked to antibiotic exposure in elderly remains inadequately understood. To investigate the association between internal exposure of antibiotics and adiposity in elderly by using a biomonitoring method. We included 990 participants (≥ 60 years) from the baseline survey of the Cohort of Elderly Health and Environment Controllable Factors in Lu’an city, China, from June to Sept. 2016. Forty-five antibiotics and two metabolites in urine were monitored through liquid chromatog.-electrospray tandem mass spectrometry (HPLC-MS/MS). Creatinine-corrected urinary concentrations were used to assess antibiotic exposure levels. Body mass index (BMI), waist circumference (WC) and body fat percentage (BFP) were used as indicators of adiposity. Multiple linear regression and binary logistic regression analyses were used to analyze the association of antibiotic concentrations with obesity-related indexes. Subsequently, a gender-stratified anal. was performed. Of the included elderly, 50.7% were defined as having overweight/obesity, 59.8% as having central preobesity/obesity, and 37.5% as having slightly high/high BFP. Linear regression anal. revealed that a 1-unit increase in the logarithmic transformation of norfoxacin concentrations was related with an increase of 0.29 kg/ m² (95% CI: 0.02-0.04), 0.99 cm (95% CI: 0.24-1.75), and 0.69% (95% CI: 0.21-1.17) in BMI, WC, and BFP, resp. Compared with the control group, exposure to doxycycline (tertile 2: odds ratio, 2.06 [95% CI: 1.12-3.76]) and norfloxacin (tertile 2: 2.13 [1.05-4.29]; tertile 3: 2.07 [1.03-4.17]) had BMI-based overweight/obesity risk. Addnl., ciprofloxacin (tertile 2: 2.06 [1.12-3.76]), norfloxacin (tertile 3: 2.95 [1.34-6.49]), and florfenicol (tertile 3:1.84 [1.07-3.14]) were related to WC-based central preobesity/obesity risk. Norfoxacin (tertile 3: 2.54 [1.23-5.24]) was pos. associated with a slightly high/high BFP risk. Gender-stratified anal. demonstrated an increased adiposity risk in women compared with men. Our research provided an evidence that exposure to specific types of antibiotics (tetracyclines and fluoroquinolones) probably from the food chain contributed to obesity in elderly. Prospective cohort studies with larger sample size are warranted to explore the causation. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Electric Literature of C11H12N4O3S).

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. 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.Electric Literature of C11H12N4O3S

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells was written by Faudone, Giuseppe;Bischoff-Kont, Iris;Rachor, Lea;Willems, Sabine;Zhubi, Rezart;Kaiser, Astrid;Chaikuad, Apirat;Knapp, Stefan;Fuerst, Robert;Heering, Jan;Merk, Daniel. And the article was included in Journal of Medicinal Chemistry in 2021.Category: pyrimidines This article mentions the following:

The ligand-sensing transcription factor tailless homolog (TLX, NR2E1) is an essential regulator of neuronal stem cell homeostasis with appealing therapeutic potential in neurodegenerative diseases and central nervous system tumors. However, knowledge on TLX ligands is scarce, providing an obstacle to target validation and medicinal chem. To discover TLX ligands, we have profiled a drug fragment collection for TLX modulation and identified several structurally diverse agonists and inverse agonists of the nuclear receptor. Propranolol evolved as the strongest TLX agonist and promoted TLX-regulated gene expression in human glioblastoma cells. Structure-activity relationship elucidation of propranolol as a TLX ligand yielded a structurally related neg. control compound In functional cellular experiments, we observed an ability of propranolol to counteract glioblastoma cell proliferation and migration, while the neg. control had no effect. Our results provide a collection of TLX modulators as initial chem. tools and set of lead compounds and support therapeutic potential of TLX modulation in glioblastoma. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Category: pyrimidines).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) 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. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis and characterization of antitubercular triazine-chalcone hybrid molecules was written by Rawat, Aman;Kaur, Atinder;Surjit;Kaur, Harpreet. And the article was included in Asian Journal of Chemistry in 2017.Category: pyrimidines This article mentions the following:

A series of 1,3,5-triazine-chalcone hybrid mols. I [R = H, MeO, C₆H₅-CH₂-O, etc.], II [R = H, CN, Cl, etc.] and III [R = H, MeO, Cl, etc.] were synthesized and evaluated in-vitro for Mycobacterium tuberculosis H37Rv inhibitory potency using Alamar blue assay and the activity expressed as the min. inhibitory concentration (MIC) in μg/mL. The antitubercular activity screening data revealed that di-Ph propen-2-one and compound II [R = H] demonstrated comparatively the most potent inhibitory activity, with MIC value 1.6 μg/mL. Most of the compounds I, II and III displayed significantly promising activity. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Category: pyrimidines).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pollution characteristics of livestock faeces and the key driver of the spread of antibiotic resistance genes was written by Yue, Zhengfu;Zhang, Jing;Zhou, Zhigao;Ding, Changfeng;Wan, Liping;Liu, Jia;Chen, Liumeng;Wang, Xingxiang. And the article was included in Journal of Hazardous Materials in 2021.Product Details of 1220-83-3 This article mentions the following:

The increasing prevalence of antibiotic resistance genes (ARGs) in livestock and poultry feces has attracted considerable amounts of attention. However, in the actual breeding environment, the key driver of the spread of ARGs and which bacteria are involved remain unclear. This study investigated 19 antibiotics and 4 heavy metals in 147 animal feces. The results showed that piglet feces exhibited the highest levels of antibiotics and heavy metals. Twelve ARGs, 4 mobile genetic elements (MGEs) and bacterial communities of piglet feces from 6 pig farms were further assessed to determine the key driver and relevant mechanism of the spread of ARGs. Sulfonamides (SAs) explained 36.5% of the variance (P < 0.05) of the bacterial community and were significantly related to 8 genes (P < 0.01), indicating that SAs dominated the spread of ARGs and should be tightly supervised. Structural equation modeling (SEM) indicated that SAs increased the abundance of ARGs via two pathways: horizontal transfer of ARGs (involving 10 genera) and vertical transfer of ARGs (involving 26 genera). These results improve our understanding of the potential hosts involved in the spread of ARGs, suggesting that monitoring of the above potential hosts is also important in animal feeding practice. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Product Details of 1220-83-3).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) 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. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Product Details of 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia