61323-64-6Relevant articles and documents
Chlorine-containing compound and application thereof as antifungal drug
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Paragraph 0041-0050, (2021/05/12)
The invention discloses a chlorine-containing compound and application thereof as an antifungal drug. The invention claims to protect a compound as shown in a formula I or pharmaceutically acceptable salts, esters and solvates thereof. In the formula I, R is -NH2 or -N=C(CH3)2. Compared with itraconazole, fluconazole and amphotericin B, the compound as shown in the formula I provided by the invention has a smaller MIC value, which shows that the compound has a more excellent antifungal effect.
Unique Sulfur-Aromatic Interactions Contribute to the Binding of Potent Imidazothiazole Indoleamine 2,3-Dioxygenase Inhibitors
Peng, Yi-Hui,Liao, Fang-Yu,Tseng, Chen-Tso,Kuppusamy, Ramajayam,Li, An-Siou,Chen, Chi-Han,Fan, Yu-Shiou,Wang, Sing-Yi,Wu, Mine-Hsine,Hsueh, Ching-Cheng,Chang, Jia-Yu,Lee, Lung-Chun,Shih, Chuan,Shia, Kak-Shan,Yeh, Teng-Kuang,Hung, Ming-Shiu,Kuo, Ching-Chuan,Song, Jen-Shin,Wu, Su-Ying,Ueng, Shau-Hua
, p. 1642 - 1659 (2020/03/17)
Indoleamine 2,3-dioxygenase (IDO1) inhibitors are speculated to be useful in cancer immunotherapy, but a phase III clinical trial of the most advanced IDO1 inhibitor, epacadostat, did not meet its primary end point and was abandoned. In previous work, we identified the novel IDO1 inhibitor N-(4-chlorophenyl)-2-((5-phenylthiazolo[2,3-c][1,2,4]triazol-3-yl)thio)acetamide 1 through high-throughput screening (HTS). Herein, we report a structure-activity relationship (SAR) study of this compound, which resulted in the potent IDO1 inhibitor 1-(4-cyanophenyl)-3-(3-(cyclopropylethynyl)imidazo[2,1-b]thiazol-5-yl)thiourea 47 (hIDO IC50 = 16.4 nM). X-ray cocrystal structural analysis revealed that the basis for this high potency is a unique sulfur-aromatic interaction network formed by the thiourea moiety of 47 with F163 and F226. This finding is expected to inspire new approaches toward the discovery of potent IDO1 inhibitors in the future.
Novel one-pot expeditious synthesis of 2,4-disubstituted thiazoles through a three-component reaction under solvent free conditions
Sujatha, Kodam,Vedula, Rajeswar Rao
, p. 302 - 308 (2018/02/09)
An expeditious one pot method has been developed for the synthesis of 2,4-disubstituted thiazoles under solvent free conditions via a multicomponent approach. Substituted thiazoles were synthesized with high yields by the reaction of cyclic ketones, thios