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Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives
Department of Pharmacology and Therapeutics, College of Medicine and Health Sciences, UAE University, Al-Ain, P.O. Box 17666, United Arab Emirates
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: 8 October 2011; in revised form: 31 October 2011 / Accepted: 7 November 2011 / Published: 9 November 2011
Abstract: A new series of 1,3-thiazole and benzo[d]thiazole derivatives 10–15 has been developed, characterized, and evaluated for in vitro antimicrobial activity at concentrations of 25–200 μg/mL 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 11 and 12 showed notable antibacterial and antifungal activities at higher concentrations (125–200 μg/mL), whereas benzo[d]thiazole derivatives 13 and 14 were found to display significant antibacterial or antifungal activity (50–75 μg/mL) against the Gram+ve, Gram–ve bacteria, or fungal cells used in the present study. In addition, a correlation between calculated and determined partition coefficient (log P) was established which allows future development of compounds within this series to be carried out based on calculated log P values. Moreover, compounds 13 and 14 show that the optimum logarithm of partition coefficient (log P) should be around 4.
Keywords: synthesis; antimicrobial evaluation; 1,3-thiazoles; benzo[d]thiazoles; partition coefficient
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Sadek, B.; Al-Tabakha, M.M.; Fahelelbom, K.M.S. Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives. Molecules 2011, 16, 9386-9396.
Sadek B, Al-Tabakha MM, Fahelelbom KMS. Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives. Molecules. 2011; 16(11):9386-9396.
Sadek, Bassem; Al-Tabakha, Moawia Mohammad; Fahelelbom, Khairi Mustafa Salem. 2011. "Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives." Molecules 16, no. 11: 9386-9396.