Synthesis of 2‐aryl‐ and 2‐haloarylbenzimidazole‐n1‐acetamido conjugates and a preliminary evaluation of their antifungal properties

Abdel‐Wahab, Sherief M. and Abdelsamii, Zakaria K. and Abdel‐Fattah, Hanan A. and Abdallah S., El‐Etrawy and Dawe, Louise N. and Swaroop, T. R. and Georghiou, Paris E. (2018) Synthesis of 2‐aryl‐ and 2‐haloarylbenzimidazole‐n1‐acetamido conjugates and a preliminary evaluation of their antifungal properties. Chemistryselect, 3 (28). pp. 8106-8110. ISSN 2365-6549

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Official URL: https://doi.org/10.1002/slct.201801151

Abstract

A series of new 2‐arylbenzimidazole‐N‐1 acetamido conjugates have been synthesized and characterized. Their antifungal activities were evaluated against fluconazole‐resistant C. albicans and A. fumigatus by the inhibition zone technique and were compared with the standard amphotericin B. Minimum inhibitory concentrations were determined for the most potent compounds, after preliminary structure‐activity analysis. Based upon these results a sub‐set of twelve ethylglycinyl ester conjugates bearing fluoro, chloro or bromo substituents on the 2‐phenyl moiety were examined for structure‐activity relationships using an agarose diffusion method employing a hypersensitive Sacharomyces cerevisiae strain. None of these compounds however showed significant activity at the concentrations tested. Single‐crystal X‐ray determinations were conducted on two of the newly synthesized compounds and were compared with DFT computational analysis.

Item Type: Article
Subjects: C Chemical Science > Organic Chemistry
Divisions: Department of > Organic Chemistry
Depositing User: Manjula P Library Assistant
Date Deposited: 08 Jul 2019 09:44
Last Modified: 21 Jun 2022 07:22
URI: http://eprints.uni-mysore.ac.in/id/eprint/4885

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