30095-56-8Relevant academic research and scientific papers
Synthesis and anticancer activity of novel 2-alkylthio-4-amino-5-(thiazol-2-YL)pyrimidines
Bunev, Alexander S.,Khochenkov, Dmitry A.,Khochenkova, Yulia A.,Machkova, Yulia S.,Varakina, Elena V.,Gasanov, Rovshan E.,Troshina, Marina A.,Avdyakova, Olga S.
supporting information, p. 2521 - 2527 (2021/06/25)
A series of new fist-time synthesized of thiazolyl-substituted 4-aminopyrimidine was obtained on the basis of a two-stage process including thioamidation of 4-amino-5-cyanopyrimide followed by one-pot acylation and Hantzsch synthesis in good yield (52–77%
A kind of two-thiazoline ketone compounds and pharmaceutical compositions thereof and use thereof (by machine translation)
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Paragraph 0129; 0130; 0131; 0133, (2017/01/17)
The invention provides general formula (I) indicated by the thiazoline ketone compounds and pharmaceutical compositions thereof and use thereof. The compounds can be combined with the bromodomain domain of the protein, thereby adjusting the downstream signal path, to play a particular function, can be used for treating the relevant domain protein in the bromodomain of various diseases. Such compounds can be interference has Brd4 bromodomain domain with the acetylated histone binding, and then lower the oncogene c - the ventilating cabins and its related target gene transcription, so that it may be effective for treating the tumor. (by machine translation)
Identification of novel 2-aminothiazole conjugated nitrofuran as antitubercular and antibacterial agents
Ran, Kai,Gao, Chao,Deng, Hongxia,Lei, Qian,You, Xinyu,Wang, Ningyu,Shi, Yaojie,Liu, Zhihao,Wei, Wei,Peng, Cuiting,Xiong, Lu,Xiao, Kunjie,Yu, Luoting
supporting information, p. 3669 - 3674 (2016/07/21)
The emergence of antibiotic resistant pathogens is an ongoing main problem in the therapy of bacterial infections. In order to develop promising antitubercular and antibacterial lead compounds, we designed and synthesized a new series of derivatives of 2-aminothiazole conjugated nitrofuran with activities against both Mycobacterium tuberculosis and Staphylococcus aureus. Eight compounds 12e, 12k, 12l, 12m, 18a, 18d, 18e, and 18j emerged as promising antitubercular agents. Structure–activity relationships (SARs) were discussed and showed that the derivatives substituted at the position-3 of benzene of 5-nitro-N-(4-phenylthiazol-2-yl)furan-2-carboxamide exhibited superior potency. The most potent compound 18e, substituted with benzamide at this position, displayed minimum inhibitory concentrations (MICs) of 0.27 μg/mL against Mtb H37Ra and 1.36 μg/mL against S. aureus. Furthermore, compound 18e had no obvious cytotoxicity to normal Vero cells (IC50= 50.2 μM). The results suggest that the novel scaffolds of aminothiazole conjugated nitrofuran would be a promising class of potent antitubercular and antimicrobial agents.
Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists
Zhang, Yu-Juan,Shen, Liu-Lan,Cheon, Hyae-Gyeong,Xu, Yong-Nan,Jeong, Jin-Hyun
, p. 588 - 599 (2014/06/09)
In this study, a series of fused-heterocyclic derivatives were systematically designed and synthesized using an efficient route, and evaluated in terms of GLP-1R agonist activity. We employed short synthetic steps and reactions that are tolerant of the presence of various functional groups and suitable for parallel operations to enable the rapid generation of libraries of diverse and structurally complex small molecules. Of the compounds synthesized, 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a] pyridin-2-yl)phenyl methanesulfonate (8e) was the most potent agonist with an EC50 of 7.89 μM, and thus is the compound with the greatest potential for application. These findings represent a valuable starting point for the design and discovery of small-molecule GLP-1R agonists that can be administered orally.
Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain
Zhao, Lele,Cao, Danyan,Chen, Tiantian,Wang, Yingqing,Miao, Zehong,Xu, Yechun,Chen, Wuyan,Wang, Xin,Li, Yanlian,Du, Zhiyan,Xiong, Bing,Li, Jian,Xu, Chunyan,Zhang, Naixia,He, Jianhua,Shen, Jingkang
, p. 3833 - 3851 (2013/07/11)
Recognizing acetyllysine of histone is a vital process of epigenetic regulation that is mediated by a protein module called bromodomain. To contribute novel scaffolds for developing into bromodomain inhibitors, we utilize a fragment-based drug discovery approach. By successively applying docking and X-ray crystallography, we were able to identify 9 fragment hits from diffracting more than 60 crystals. In the present work, we described four of them and carried out the integrated lead optimization for fragment 8, which bears a 2-thiazolidinone core. After several rounds of structure guided modifications, we assessed the druggability of 2-thiazolidinone by modulating in vitro pharmacokinetic studies and cellular activity assay. The results showed that two potent compounds of 2-thiazolidinones have good metabolic stability. Also, the cellular assay confirmed the activities of 2-thiazolidinones. Together, we hope the identified 2-thiazolidinone chemotype and other fragment hits described herein can stimulate researchers to develop more diversified bromodomain inhibitors.
2-(4-BENZOYL-1-PIPERIDYL)-1-PHENYLALKANOL DERIVATIVES
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, (2008/06/13)
Compound of general formula I STR1 in which R is hydrogen, R 1 is unsubstituted phenyl, 4-methoxy-3,5-dimethylphenyl or phenyl substituted at one of the 2-, 3-or 4-positions by halogen, C 1-4 alkyl, C 1-4 alkoxy, hydroxy, benzyloxy, trifluoromethyl, cyano, nitro, amino, acetylamino, methylthio, methylsulphonyl or aminosulphonyl and R 2 is unsubstituted phenyl, 2,4,6-trimethoxyphenyl or phenyl substituted at either the 3-or the 4-positions by fluorine, chlorine, methyl or methoxy, or an acid addition salt thereof.
Novel crotonanilides
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, (2008/06/13)
Novel crotonanilides of the formula STR1 wherein Z is selected from the group consisting of --O-- and --S--, R is selected from the group consisting of alkyl of 1 to 6 carbon atoms and optionally substituted phenyl, X and Y are individually selected from the group consisting of hydrogen, halogen, lower alkyl of 1 to 6 carbon atoms optionally substituted with at least one halogen, alkoxy of 1 to 3 carbon atoms, alkylthio and alkylsulfinyl of 1 to 6 carbon atoms, acyl of an organic carboxylic acid of 1 to 6 carbon atoms, --NO2 and --CF3, R1 is selected from the group consisting of hydrogen, chlorine, bromine, alkoxycarbonyl with 1 to 6 alkyl carbon atoms, nitro and alkylthio, alkylsulfinyl and alkylsulfonyl of 1 to 3 alkyl carbon atoms and R2 is alkyl of 1 to 6 carbon atoms, said compounds existing in the form of their E or Z isomers or mixtures thereof and having herbicidal properties.
6-Substituted amino phenyl-2,3,5,6-tetrahydro[2,1-b]thiazoles
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, (2008/06/13)
The preparation of dl and l compounds of the type 6-(mono and di-substituted phenyl)-5,6-dihydro or 2,3,5,6-tetrahydroimidazo[2,1-b]thiazoles and the pharmaceutically acceptable salts thereof, is described. The use of said compounds for treating helminthiasis in warm-blooded animals is also described.
Method of using 6-substituted amino phenyl-2,3,5,6-tetra-hydro[2,1-b]thiazoles for controlling gastrointestinal nematodes
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, (2008/06/13)
The preparation of compounds of the type 6-(mono substituted phenyl)-5,6-dihydro or 2,3,5,6-tetrahydroimidazo[2,1-b]thiazoles and the pharmaceutically acceptable salts thereof, is described. The use of said compounds for treating helminthiasis in warm-blooded animals is also described.
