693217-22-0Relevant academic research and scientific papers
Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates
Zou, Yan,Yu, Shichong,Li, Renwu,Zhao, Qingjie,Li, Xiang,Wu, Maocheng,Huang, Ting,Chai, Xiaoxun,Hu, Honggang,Wu, Qiuye
, p. 366 - 374 (2014/02/14)
A series of 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl) propyl dithiocarbamates as new analogs of fluconazole were synthesized and their antifungal activities were evaluated. Among these compounds, 2a-f and 3a-q exhibited higher activities than fluconazole against nearly all fungi tested except Aspergillus fumigatus. Noticeably, the in vitro biological activities of 2b, 3a, 3c, 3h-k, and 3o-q against Candida species were much better than those of fluconazole and ketoconazole. Also, 2a-d, 3a-d, 3e-f, 3h-k, 3p and 3q showed higher activities against A. fumi than fluconazole. Computational docking experiments indicated that the inhibition of CYP51 involved a coordination bond with iron of the heme group, the hydrophilic H-bonding region, the hydrophobic region, and the narrow hydrophobic cleft.
Synthesis and cytotoxicity screening of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones
Cao, Sheng-Li,Guo, Yan-Wen,Wang, Xian-Bo,Zhang, Mei,Feng, Yu-Ping,Jiang, Yu-Yang,Wang, Yue,Gao, Qian,Ren, Jian
experimental part, p. 182 - 189 (2009/05/26)
A new series of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones were synthesized via a five-steps procedure starting from 2-amino-5-methylbenzoic acid. The cytotoxicity of the resulting compounds against A-549 (human lung ca
