Synthesize and evaluate some phenyl substituted thiazole linked 1, 2, 4-triazole derivatives as antimicrobial agents.

Compounds containing 1, 2, 4-triazole moieties are widely used as antimicrobial and antifungal agents whereas thiazole is another heterocyclic ring exhibiting various pharmacological actions. It is interesting to incorporate different bioactive pharmacophores in the same molecular framework to examine cumulative effect exerted by the moiety. This hypothesis was applied in research work by having triazole and thiazole in the same molecular framework.

The present work was mainly focused on synthesis of some 1, 2, 4-triazole derivatives linking with phenyl substituted thiazole nucleus and their evaluation for biological activity. The compounds (8a-8j) were synthesized as per design scheme and elucidated their structures using different spectroscopic data of IR, 1HNMR, 13CNMR & mass spectroscopy. These synthesized derivatives were evaluated for their antibacterial activity using broth dilution assay. Further, mechanism of action of test compounds was examined using protein leakage assay.

All the spectral data were confirmed the synthesis of phenyl substituted thiazole linked 1, 2, 4- triazole derivatives and some of them exhibited significant antimicrobial activity.

Amongst all compound 8c showed most potent activity with lowest IC50 values 180 μg/ml and 120 μg/ml against S. aureus & amp; B. cereus respectively. Whereas compound 8j demonstrated strong inhibitory activities only against negative strains P. aeruginosa and E. coli with lowest IC50 values 240 μg/mL and 200μg/mL respectively.

合成并评估一些苯基取代的噻唑连接的 1, 2, 4-三唑衍生物作为抗菌剂。

含有 1, 2, 4-三唑部分的化合物被广泛用作抗微生物剂和抗真菌剂，而噻唑是另一种具有多种药理作用的杂环。在同一分子框架中加入不同的生物活性药效团以检查该部分发挥的累积效应是很有趣的。通过在相同的分子框架中具有三唑和噻唑，将这一假设应用于研究工作。

目前的工作主要集中在一些与苯基取代的噻唑核相连的1, 2, 4-三唑衍生物的合成及其生物活性评价。根据设计方案合成化合物(8a-8j)，并使用IR、1HNMR、13CNMR和质谱的不同光谱数据阐明它们的结构。使用肉汤稀释试验评估这些合成衍生物的抗菌活性。此外，使用蛋白质渗漏试验检查了测试化合物的作用机制。

所有光谱数据都证实了苯基取代的噻唑连接的 1, 2, 4- 三唑衍生物的合成，其中一些表现出显着的抗菌活性。

在所有化合物 8c 中，化合物 8c 对金黄色葡萄球菌和金黄色葡萄球菌的活性最强，IC50 值最低，分别为 180 μg/ml 和 120 μg/ml。B.蜡状分别。而化合物 8j 仅对阴性菌株铜绿假单胞菌和大肠杆菌表现出强抑制活性，最低 IC50 值分别为 240 μg/mL 和 200 μg/mL。