synthesis, characterization, and antimicrobial evaluation of oxadiazole congeners合成、表征和抗菌oxadiazole同系物的评价.pdfVIP

Molecules 2011, 16, 4339-4347; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules 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; E-Mail: staff.bassem.s@alainuniversity.ac.ae; Tel.: +971-37-611-185; Fax: +971-37-611-198. Received: 13 April 2011; in revised form: 10 May 2011 / Accepted: 19 May 2011 / Published: 25 May 2011 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, respectiv