Synthesis,antimicrobial, antiquorum-sensing and cytotoxic activities of new series of benzothiazole derivatives

被引：0

作者：

Moustafa T.Gabr ^{[1
,2
]}

Nadia S.El-Gohary ^{[1
]}

Eman R.El-Bendary ^{[1
]}

Mohamed M.El-Kerdawy ^{[1
]}

Nanting Ni ^{[2
]}

Mona I.Shaaban ^{[3
,4
]}

机构：

[1] Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University

[2] Department of Chemistry, Georgia State University

[3] Department of Microbiology, Faculty of Pharmacy, Mansoura University

[4] Department of Microbiology, College of Pharmacy, Taibah University

来源：

Chinese Chemical Letters | 2015年 / 26卷 / 12期

关键词：

Benzothiazoles; Antimicrobial activity; Antiquorum-sensing activity; Cytotoxic activity; In silico studies;

D O I：

暂无

中图分类号：

TQ465 [抗菌素制造]; O626.25 [间硫氮茂（噻唑）];

学科分类号：

070303 ; 081704 ; 100705 ;

摘要：

New series of benzothiazole derivatives were designed and synthesized. The newly synthesized compounds were screened for their antibacterial activity against Escherichia coli, Staphylococcus aureus and Bacillus cereus. Compounds 6j and 6o showed the highest activity against E. coli and S. aureus. The antifungal activity of these compounds was also tested against Candida albicans and Aspergillus fumigatus293. Compounds 4c, 4g and 6j exhibited the highest activity against C. albicans. In addition, compounds4 a and 6j displayed promising activity against A. fumigatus 293. The same compounds were examined for their antiquorum-sensing activity against Chromobacterium violaceum ATCC 12472, whereas compounds4 a, 6j and 6p showed moderate activity. The in vitro cytotoxicity testing of the synthesized compounds was performed against cervical cancer(Hela) and kidney fibroblast cancer(COS-7) cell lines. Results indicated that all tested compounds have IC50 values >50 mmol/L against both cell lines. Molecular properties, toxicities, drug-likeness, and drug score profiles of compounds 4a–c, 5a, 6g,h, 6j, 6l, 6o and7 c,d were also assessed.

引用

页码：1522 / 1528

页数：7

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