Synthesis of novel 2-aminobenzothiazole derivatives as potential antimicrobial agents with dual DNA gyrase/topoisomerase IV inhibition

被引：23

作者：

Ismail, Magda M. F. ^{[1
]}

Abdulwahab, Hanan Gaber ^{[1
]}

Nossier, Eman Samir ^{[1
]}

El Menofy, Nagwan Galal ^{[2
]}

Abdelkhalek, Basma Abdelhameed ^{[1
]}

机构：

[1] Al Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Chem, Cairo, Egypt

[2] Al Azhar Univ, Fac Pharm Girls, Dept Microbiol & Immunol, Cairo, Egypt

来源：

BIOORGANIC CHEMISTRY | 2020年 / 94卷

关键词：

Benzothiazole; Antimicrobial; DNA gyrase; Topoisomerase IV; Dual inhibitor; Multi-drug resistant; MRSA; BIOLOGICAL EVALUATION; GYRASE; DISCOVERY;

D O I：

10.1016/j.bioorg.2019.103437

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：

Novel benzothiazole-based compounds were designed and synthesized as potential antimicrobial agents with dual DNA gyrase/topoisomerase IV inhibitory activity. The structures of the newly synthesized compounds were established on the basis of spectral (IR, NMR, MS) and elemental analyses. Most of the studied compounds possessed significant antimicrobial activity against tested bacteria and fungi. Compounds 4b and 7a were much more potent than reference standard ciprofloxacin against methicillin-resistant Staphylococcus aureus (MRSA) and a multi-drug resistant clinical isolate of Enterococcus faecium. Moreover, 7a was equipotent to nystatin against clinical isolate of Candida albicans. Both 4b and 7a inhibited DNA gyrase and topoisomerase IV at low micromolar levels and also displayed safety profiles much better than that of novobiocin in cytotoxicity assay.

引用

页数：14

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