Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives

被引:42
|
作者
Sadek, Bassem [1 ]
Al-Tabakha, Moawia Mohammad [2 ]
Fahelelbom, Khairi Mustafa Salem [2 ]
机构
[1] UAE Univ, Coll Med & Hlth Sci, Dept Pharmacol & Therapeut, Al Ain, U Arab Emirates
[2] Al Ain Univ Sci & Technol, Coll Pharm, Dept Pharmaceut Sci, Al Ain, U Arab Emirates
关键词
synthesis; antimicrobial evaluation; 1,3-thiazoles; benzo[d]thiazoles; partition coefficient; ANTITUMOR BENZOTHIAZOLES; ANTIBACTERIAL ACTIVITY; BIOLOGICAL-PROPERTIES; PENICILLIN; INHIBITORS; POTENT; 2-(4-AMINOPHENYL)BENZOTHIAZOLES; CEFTRIAXONE; MENINGITIS; RESISTANT;
D O I
10.3390/molecules16119386
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
收藏
页码:9386 / 9396
页数:11
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