Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents

被引：91

作者：

Ertan, Tugba ^{[1
]}

Yildiz, Ilkay ^{[1
]}

Tekiner-Gulbas, Betul ^{[1
]}

Bolelli, Kayhan ^{[1
]}

Temiz-Arpaci, Ozlem ^{[1
]}

Ozkan, Semiha ^{[2
]}

Kaynak, Fatma ^{[2
]}

Yalcin, Ismail ^{[1
]}

Aki, Esin ^{[1
]}

机构：

[1] Ankara Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey

[2] Gazi Univ, Fac Pharm, Dept Pharmaceut Microbiol, TR-06330 Ankara, Turkey

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 02期

关键词：

Antibacterial activity; Antifungal activity; Benzoxazoles; 2D-QSAR; REVERSE-TRANSCRIPTASE INHIBITOR; TOPOISOMERASE-II INHIBITORS; MICROBIOLOGICAL ACTIVITY; HETEROCYCLIC-COMPOUNDS; ANTIBIOTIC-RESISTANCE; CYTOTOXIC METABOLITE; DERIVATIVES; BENZIMIDAZOLES; ANALOGS; 3D-QSAR;

D O I：

10.1016/j.ejmech.2008.04.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 5(or 6)-nitro/amino-2-(substituted phenyl/benzyl)benzoxazole derivatives (1a-1m, 2a-21) were synthesized and evaluated for antibacterial and antifungal activities against Staphylococcus aureus, Bacillus subtilis, Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, Candida albicans and their drug-resistant isolate. Microbiological results indicated that the synthesized compounds possessed a broad spectrum of activity against the tested microorganisms at MIC values between >400 and 12.5 mu g/ml. The results against B. subtilis, P. aeruginosa, drug-resistant B. subtilis, drug-resistant E. coli, and C. albicans isolate for these kinds of structures are quite encouraging. The 2D-QSAR analysis of a set of newly and previously synthesized benzoxazoles tested for growth inhibitory activity against B. subtilis ATCC 6633 was performed by using the multivariable regression analysis. The activity contributions for substituent effects of these compounds were determined from the correlation equation for predictions of the lead optimization. (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：501 / 510

页数：10

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