Synthesis, potent anti-staphylococcal activity and QSARs of some novel 2-anilinobenzazoles
European Journal of Medicinal Chemistry, vol.43, no.7, pp.1390-1402, 2008 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 43 Issue: 7
- Publication Date: 2008
- Doi Number: 10.1016/j.ejmech.2007.10.009
- Journal Name: European Journal of Medicinal Chemistry
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Page Numbers: pp.1390-1402
- Keywords: anilinobenzimidazole, anilinobenzothiazole, anilinobenzoxazole, anti-staphy lococcal activity, k(w) capacity factors, QSAR, PERFORMANCE LIQUID-CHROMATOGRAPHY, ANTIMICROBIAL ACTIVITY, ACID-DERIVATIVES, LOG KW, LIPOPHILICITY, HYDROPHOBICITY, VALUES
- Lokman Hekim University Affiliated: No
Abstract
Synthesis and anti-staphylococcal activity of a number of substituted 2-anilinobenzimidazoles, benzothiazoles and benzoxazoles are reported. The anti-staphylococcal activities were evaluated in standard in vitro MIC assay method. While anilinobenzimidazole derivatives 11-45 showed very potent anti-staphylococcal activities (greatest activity with an MIC value of 0.095 μg/mL), none of the 2-anilinobenzothiazoles and benzoxazole derivatives exhibited inhibitory activity. QSAR analysis of the anilinobenzimidazoles was studied on the relationship between the anti-staphylococcal activity (MIC in μg/ml) and extrapolated log kw values. © 2007 Elsevier Masson SAS. All rights reserved.