Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents

被引：11
|
作者：
Wang, Apeng [1 ]
Xu, Shijie [1 ]
Chai, Yun [1 ,2 ]
Xia, Guimin [1 ]
Wang, Bin [3 ]
Lv, Kai [1 ]
Wang, Dan [1 ]
Qin, Xiaoyu [1 ]
Jiang, Bin [1 ,4 ]
Wu, Wenhao [1 ,4 ]
Liu, Mingliang [1 ]
Lu, Yu [3 ]
机构：
[1] Chinese Acad Med Sci & Peking Union Med Coll, Inst Med Biotechnol, Beijing 100050, Peoples R China
[2] Northwestern Polytech Univ, Inst Med Res, 127 West Youyi Rd, Xian 710072, Peoples R China
[3] Med Univ, Beijing Chest Hosp, Capital Coll Pharm,Dept Pharmacol, Beijing TB & Thorac Tumor Res Inst,Beijing Key La, Beijing 100149, Peoples R China
[4] Hebei Med Univ, Shijiazhuang 050017, Hebei, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2022年 / 53卷
关键词：
Nitrofuran-1; 4-oxadiazole hybrids; Antitubercular activity; Synthesis; DRUG DISCOVERY; TUBERCULOSIS; ANALOGS; IDENTIFICATION; DERIVATIVES; EFFICACY;
D O I：
10.1016/j.bmc.2021.116529
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Three series of novel nitrofuran-1,3,4-oxadiazole hybrids were designed and synthesized as new anti-TB agents. The structure activity relationship study indicated that the linkers and the substituents on the oxadiazole moiety greatly influence the activity, and the substituted benzenes are more favoured than the cycloalkyl or heterocyclic groups. Besides, the optimal compound in series 2 was active against both MTB H37Rv strain and MDR-MTB 16883 clinical isolate and also displayed low cytotoxicity, low inhibition of hERG and good oral PK, indicating its promising potential to be a lead for further structural modifications.
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页数：10
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