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

Abstract：

: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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Ismail MMF,Abdulwahab HG,Nossier ES,El Menofy NG,Abdelkhalek BA

doi

10.1016/j.bioorg.2019.103437

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

103437

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)31346-X

journal_volume

94

pub_type

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