Department of Pharmacology and Therapeutics, College of Medicine and Health Sciences, UAE University, Al-Ain, P.O. Box 17666, United Arab Emirates.
Molecules. 2011 Nov 9;16(11):9386-96. doi: 10.3390/molecules16119386.
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.
已经开发、表征了一系列新的 1,3-噻唑和苯并[d]噻唑衍生物 10-15，并通过杯碟法在 25-200μg/mL 浓度下评估了它们对革兰氏阳性菌（如耐甲氧西林金黄色葡萄球菌（MRSA））、革兰氏阴性菌（如大肠杆菌（E. coli））和真菌黑曲霉（A. niger）的体外抗菌活性。氧氟沙星和酮康唑（10μg/mL）分别用作抗菌和抗真菌活性的参考标准。化合物 11 和 12 在较高浓度（125-200μg/mL）下表现出显著的抗菌和抗真菌活性，而苯并[d]噻唑衍生物 13 和 14 则对革兰氏阳性、革兰氏阴性细菌或本研究中使用的真菌细胞显示出显著的抗菌或抗真菌活性（50-75μg/mL）。此外，建立了计算和测定分配系数（log P）之间的相关性，这使得可以根据计算的 log P 值来进行该系列化合物的进一步开发。此外，化合物 13 和 14 表明，最佳分配系数（log P）的对数应该在 4 左右。
