Category: pyrimidines

Ognyanov, Vassil I.; Balan, Chenera; Bannon, Anthony W.; Bo, Yunxin; Dominguez, Celia; Fotsch, Christopher; Gore, Vijay K.; Klionsky, Lana; Ma, Vu V.; Qian, Yi-Xin; Tamir, Rami; Wang, Xianghong; Xi, Ning; Xu, Shimin; Zhu, Dawn; Gavva, Narender R.; Treanor, James J. S.; Norman, Mark H. published the artcile< Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles>, Category: pyrimidines, the main research area is benzimidazole piperazinyl preparation transient receptor potential vanilloid antagonist antihyperalgesic.

The vanilloid receptor-1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel that is predominantly expressed by peripheral neurons sensing painful stimuli. TRPV1 antagonists produce antihyperalgesic effects in animal models of inflammatory and neuropathic pain. The synthesis and the structure-activity relationships of a series of 2-(4-pyridin-2-ylpiperazin-1-yl)-1H-benzo[d]imidazoles I [R1 = H, Me3SiCH2CH2OCH2, PhCH2; R2 = F, Cl, Br, F3C, Me, CN, Me3C, MeO2C, etc.; R3 = H, 4-(2-thiazolyl), 4-(4-pyridyl), 5-(4-F3CC6H4), etc.; R4 = H, Me; R5 = H, H2N, MeCHOH, H2C:CH, etc.; R6 = H, Cl, F3C, etc.] and analogs as novel TRPV1 antagonists have been described. I [R1 = H; R2 = F3C; R3 = 4-(3,4,5-F3C6H2); R4 = (R)-Me; R5 = HOCH2CHOH; R6 = Cl; (II)] was among the most potent analogs in this series. This compound was orally bioavailable in rats and was efficacious in blocking capsaicin-induced flinch in rats in a dose-dependent manner. II also reversed thermal hyperalgesia in a model of inflammatory pain, which was induced by complete Freund’s adjuvant (CFA).

Journal of Medicinal Chemistry published new progress about Analgesics. 6554-61-6 belongs to class pyrimidines, and the molecular formula is C4H2Cl2N2, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hornillo-Araujo, Ana R.; Burrell, Adam J. M.; Aiertza, Miren K.; Shibata, Takayuki; Hammond, David M.; Edmont, Dolores; Adams, Harry; Margison, Geoffrey P.; Williams, David M. published the artcile< The syntheses and properties of tricyclic pyrrolo[2,3-d]pyrimidine analogues of S6-methylthioguanine and O6-methylguanine>, Formula: C7H8N4O, the main research area is tricyclic pyrrolopyrimidine analog thioguanine methylguanine preparation; thiopyran tricyclic pyrrolopyrimidine analog thioguanine methylguanine preparation; thiepane tricyclic pyrrolopyrimidine analog thioguanine methylguanine preparation; DNA cross linking tricyclic pyrrolopyrimidine analog thioguanine methylguanine preparation; oligonucleotide pseudosubstrate DNA linking tricyclic pyrrolopyrimidine analog thioguanine methylguanine.

The syntheses of novel tricyclic pyrrolo[2,3-d]pyrimidine analogs of S6-methylthioguanine are described. The crystal structures and pKa values of these and related O6-methylguanine analogs are reported. All compounds display higher pKa values than O6-methylguanine with the sulfur-containing analogs being the more basic and exhibiting higher stability in aqueous solution In a standard substrate assay with the human repair protein O6-methylguanine-DNA methyltransferase (MGMT) only the oxygen-containing analog displayed activity.

Organic & Biomolecular Chemistry published new progress about Crystal structure. 84955-32-8 belongs to class pyrimidines, and the molecular formula is C7H8N4O, Formula: C7H8N4O.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Krasavin, Mikhail; Mujumdar, Prashant; Parchinsky, Vladislav; Vinogradova, Tatiana; Manicheva, Olga; Dogonadze, Marine published the artcile< Library of diversely substituted 2-(quinolin-4-yl)imidazolines delivers novel non-cytotoxic antitubercular leads>, COA of Formula: C4H2Cl2N2, the main research area is quinolinylimidazoline derivative preparation antitubercular antimalarial; 2-imidazoline; Antimalarial; Buchwald–Hartwig; antitubercular; microwave chemistry; non-cytotoxic; quinoline.

A novel library based on quinolin-4-ylimidazoline core was designed to incorporate a general quinoline antimicrobial pharmacophore. A synthesis of the well-characterized library of 36 compounds was achieved using the Pd-catalyzed Buchwald-Hartwig-type imidazoline arylation chem. developed earlier. Compounds were tested for biol. activity and were found to possess no antimalarial activity. However, the library delivered two promising antitubercular leads, which are non-cytotoxic and can be further optimized with respect to antimycobacterial potency.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antimalarials. 6554-61-6 belongs to class pyrimidines, and the molecular formula is C4H2Cl2N2, COA of Formula: C4H2Cl2N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Liu, Zhiqing; Ai, Jing; Peng, Xia; Song, Zilan; Wu, Kui; Zhang, Jing; Yao, Qizheng; Chen, Yi; Ji, Yinchun; Yang, Yanhong; Geng, Meiyu; Zhang, Ao published the artcile< Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities>, Formula: C6H2Cl2N2S, the main research area is arylaminopyrimidine preparation SAR cMet ALK multikinase inhibitor antitumor; 2,4-diarylaminopyrimidine analogues; C1-Substituted-N3-benzazepine; c-Met/ALK dual inhibitor; structure repurposing.

By repurposing a typical dopamine D1/D5 receptor agonist motif, C1-substituted-N3-benzazepine or benzazecine, into the classical RTK inhibitor 2,4-diaminopyrimidine skeleton, a series of new 2,4-diarylaminopyrimidine analogs (DAAPalogues) were developed. Two compounds were identified possessing high potency against both c-Met and ALK kinases. Compound (I) displayed appreciable antitumor efficacy at the dose of 1 mg/kg in the ALK-driven BF3/EML4-ALK xenograft mice model.

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Formula: C6H2Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Amano, Yohei; Noguchi, Masayuki; Shudo, Koichi published the artcile< Diarylamines incorporating hexahydrophenalene or octahydrobenzoheptalene as retinoid X receptor (RXR)-specific agonists>, Safety of Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is arylamino hexahydro phenalene preparation retinoid X receptor agonist; octahydro benzoheptalene arylamino preparation retinoid X receptor agonist.

A series of diarylamines I (X = CH2, R1 = H, Me; X = CH2CH2, R1 = H; Z = CH, N; R2 = H, Me, Et, cyclopropylmethyl, i-Bu, PhCH2) incorporating hexahydrophenalene or octahydrobenzoheptalene as a hydrophobic moiety was synthesized and examined for their activities towards retinoic acid receptors (RARs) and retinoid X receptors (RXRs). Most of these compounds showed agonistic activity towards RXRs, but were inactive towards RARs. These RXR-specific ligands showed synergistic activity in RARα,β ligand-induced terminal differentiation of leukemia cell line HL-60.

Chemical & Pharmaceutical Bulletin published new progress about Aromatic amines Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Safety of Ethyl 2-chloropyrimidine-5-carboxylate.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Okui, Kiyoshi; Ito, Kiyohiko; Koizumi, Masuo; Fukumoto, Keiichiro; Kametani, Tetsuji published the artcile< Syntheses of heterocyclic compounds. CDXCI. Pyrimidine derivatives. V. Abnormal condensation products of 4-amino-6-chloro-2-methoxypyrimidine with p-nitrobenzenesulfonyl chloride>, Related Products of 3286-55-3, the main research area is pyridinium pyrimidine betaines.

Condensation of 4-amino-6-chloro-2-methoxypyrimidine with p-O2NC6H4SO2Cl gave, in addition to 6-chloro-2-methoxy-4-(p-nitrobenzenesulfonamido)pyrimidine (I), two abnormal by-products, 1-[2-methoxy-4-(p-nitrobenzenesulfonamido)pyrimidin-6-yl]pyridinium N,N-betaine (II) and N-(p-nitrobenzenesulfonyl)-β-ureido-β-pyridinium arcylamide N,N-betaine (III).

Journal of Heterocyclic Chemistry published new progress about 3286-55-3. 3286-55-3 belongs to class pyrimidines, and the molecular formula is C5H6ClN3O, Related Products of 3286-55-3.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Park, Tae-Hong; Cychosz, Katie A.; Wong-Foy, Antek G.; Dailly, Anne; Matzger, Adam J. published the artcile< Gas and liquid phase adsorption in isostructural Cu3[biaryltricarboxylate]2 microporous coordination polymers>, Safety of Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is gas liquid adsorption copper isostructural biaryltricarboxylate microporous polymer; crystal structure copper carboxypyrimidinyl carboxypyridinyl isophthalate microporous coordination polymer; copper biaryltricarboxylate microporous polymer preparation gas liquid adsorption.

N-Heteroarene substitution in biphenyl-based linkers enhances the uptake of electron-rich organosulfur mols. in microporous coordination polymers (MCP). Three isostructural MCPs are prepared (Cu3L2) possessing nearly uniform surface areas from homologous biaryl tricarboxylate linkers containing Ph (biphenyltricarboxylate UMCM-150), pyrimidine (carboxypyrimidinyl-isophthalate UMCM-150N2), and pyridine (carboxypyridinyl-isophthalate UMCM-150N1) units, building the ideal system to probe linker influence upon guest adsorption. The almost identical isotherms of H2 and CO2 in these MCPs imply that the N-heteroaryl linkers in the UMCM-150 analogs do not considerably affect the gas phase adsorption behavior. The electronic nature and contact interactions with the aromatic linker play an important role to enhance interactions between the host MCP framework and the large guest organic mols. in the liquid phase.

Chemical Communications (Cambridge, United Kingdom) published new progress about Adsorption (isotherm). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Safety of Ethyl 2-chloropyrimidine-5-carboxylate.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia