Synthesis and Biological Evaluation New Imidazo[2,1-b]thiazoles

被引:0
作者
Syed, Manjoor A. [1 ]
Yiragamreddy, Padmanabha R. [1 ]
Chandrasekhar, K. B. [2 ]
机构
[1] Raghavendra Inst Pharmaceut Educ & Res RIPER, Dept Pharmaceut Chem, Chiyyedu, Anantapuramu, India
[2] JNTUA Oil Technol & Pharmaceut Res Inst, Dept Chem, Anantapuramu, Andhra Pradesh, India
关键词
Antifungal; Antitubercular; Imidazo[2,1-b]thiazoles; Docking studies; Vilsmeier-Haack reaction; MYCOBACTERIUM-TUBERCULOSIS; ANTIMYCOBACTERIAL ACTIVITIES; DERIVATIVES; INHIBITORS;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of some 36 new imidazo[2,1-b] thiazoles (4a1-a6 to 4f1-f6) was synthesized involving multi-steps method starting from commercially available 2-aminothiazole (1). All the compounds were screened for antitubercular and antifungal activity. The compounds 4a1, 4a2, 4b3, 4b4, 4d5, and 4e4 with minimum inhibitory concentration (MIC) 1.6 mu g/mL displayed very good antitubercular and 4a2, 4b4, 4c4, and 4d2 displayed very good antifungal activity with MIC 25 mu g/mL. The few active molecules were subjected to molecular docking studies against three enzymes, pantothenate synthetase, enoyl-acyl carrier protein reductase (InhA), and aminoglycoside 2'-N-acetyltransferase of Mycobacterium tuberculosis (TB), which have been validated as effective anti-TB targets. [GRAPHICS] .
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页码:329 / 338
页数:10
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