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.
Original language | English |
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Pages (from-to) | 9386-9396 |
Number of pages | 11 |
Journal | Molecules |
Volume | 16 |
Issue number | 11 |
DOIs | |
Publication status | Published - Nov 2011 |
Keywords
- 1,3-thiazoles
- Antimicrobial evaluation
- Partition coefficient
- Synthesis
- benzo[d]thiazoles
ASJC Scopus subject areas
- Analytical Chemistry
- Chemistry (miscellaneous)
- Molecular Medicine
- Pharmaceutical Science
- Drug Discovery
- Physical and Theoretical Chemistry
- Organic Chemistry