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Molecules 2011, 16(6), 4339-4347; doi:10.3390/molecules16064339

Article

Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners

Bassem Sadek*  and Khairi Mustafa Salem Fahelelbom

Department of Pharmaceutical Sciences, College of Pharmacy, Al-Ain University of Science and Technology, P.O. Box 64141, Al Ain, United Arab Emirates

* Author to whom correspondence should be addressed.

Received: 13 April 2011; in revised form: 10 May 2011 / Accepted: 19 May 2011 / Published: 25 May 2011

(This article belongs to the Section Medicinal Chemistry)

Download PDF Full-Text [176 KB, uploaded 25 May 2011 15:27 CEST]

Abstract: A series of 1,3-oxazole, 1,3-thiazole, isomeric 1,2,4-oxadiazole, 1,3,4-oxadiazole, and 1,2,3,4-tetrazole heterocycles was synthesized. All the compounds shared as a common feature the presence of a 4-hydroxyphenyl substituent. The structures of the synthesized compounds were confirmed by MS, ¹H-NMR, and elemental analysis. In vitro antimicrobial activity for all the newly synthesized compounds at concentrations of 200-25 μg/mL was evaluated against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram–ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 μg/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 15, 16, and 20 showed notable antibacterial and antifungal activities at higher concentrations (200 μg/mL), whereas 17-19 were found to display significant antibacterial or antifungal activity (25-50 μg/mL) against the Gram+ve, Gram–ve bacteria, or fungal cells used in the present study.

Keywords: 1,3-oxazole; oxadiazole congeners; 1,3-thiazole; tetrazole; antibacterial; antifungal

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