2-Aminobenzothiazole derivatives: Search for new antifungal agents

被引：96

作者：

Catalano, Alessia ^{[1
]}

Carocci, Alessia ^{[1
]}

Defrenza, Ivana ^{[1
]}

Muraglia, Marilena ^{[1
]}

Carrieri, Antonio ^{[1
]}

Van Bambeke, Francoise ^{[2
]}

Rosato, Antonio ^{[1
]}

Corbo, Filomena ^{[1
]}

Franchini, Carlo ^{[1
]}

机构：

[1] Univ Bari Aldo Moro, Dipartimento Farm Sci Farmaco, I-70125 Bari, Italy

[2] Catholic Univ Louvain, Louvain Drug Res Inst, B-1200 Brussels, Belgium

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 64卷

关键词：

Antifungal activity; 2-Aminobenzothiazole derivatives; CA-CYP51; Docking; Cytotoxicity; LANOSTEROL; 14-ALPHA-DEMETHYLASE; BIOLOGICAL EVALUATION; IN-VITRO; CANDIDA-ALBICANS; DESIGN; MEXILETINE; POTENT; CYP51; INHIBITION; BLOCKERS;

D O I：

10.1016/j.ejmech.2013.03.064

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A new series of 6-substituted 2-aminobenzothiazole derivatives were synthesized and screened in vitro as potential antimicrobials. Almost all the compounds showed antifungal activity. In particular, compounds 1n,o, designed on the basis of molecular modeling studies, were the best of the series, showing MIC values of 4-8 mu g/mL against Candida albicans, Candida parapsilosis and Candida tropicalis. None of the two compounds did show any cytotoxicity effect on human THP-1 cells. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：357 / 364

页数：8

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