Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives

作者：Sadek Bassem^*; Al Tabakha Moawia Mohammad; Fahelelbom Khairi Mustafa Salem

来源：Molecules, 2011, 16(11): 9386-9396.

DOI：10.3390/molecules16119386

• synthesis
• antimicrobial evaluation
• 1,3-thiazoles
• benzo[d]thiazoles
• partition coefficient

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 mu g/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 mu g/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 mu g/mL), whereas benzo[d] thiazole derivatives 13 and 14 were found to display significant antibacterial or antifungal activity (50-75 mu g/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.

• 出版日期2011-11