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Ultrasound assisted, VOSO4 catalyzed synthesis of 4-thiazolidinones: Antimicrobial evaluation of indazole-4-thiazolidinone derivatives
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2017-10-27 , DOI: 10.1016/j.tetlet.2017.10.070
Srinivas Angapelly , P.V. Sri Ramya , Routhu SunithaRani , C. Ganesh Kumar , Ahmed Kamal , Mohammed Arifuddin

A simple and expedient multicomponent protocol was developed to synthesize 4-thiazolidinones by employing VOSO4 as a catalyst under ultrasonic irradiation. The significant features of this protocol includes shorter reaction time, high yields, low catalyst loading, and also the catalyst can be recovered and reused up to next four cycles without significant loss in catalytic activity. All the synthesized novel indazole compounds were evaluated for their antibacterial and anti-biofilm activities. Compounds 9n, 9o and 9q showed promising activity (MIC value of 3.9 µg/mL) against K. planticola (MTCC 530). They also exhibited significant bactericidal activity against K. planticola (MTCC 530) (MBC value of 15.6 µg/mL). Additionally, 9n, 9o and 9q inhibited biofilm formation (IC50 values ranging between 20.28–20.79 μg/mL) in this organism.



中文翻译:

超声辅助VOSO 4催化合成4-噻唑烷酮:吲唑-4-噻唑烷酮衍生物的抗菌评估

通过在超声辐射下采用VOSO 4作为催化剂,开发了一种简单且方便的多组分方案以合成4-噻唑烷酮。该方案的重要特征包括较短的反应时间,高收率,较低的催化剂负载量,并且该催化剂可以回收并重复使用至下一个四个循环,而不会显着降低催化活性。对所有合成的新型吲唑化合物的抗菌和抗生物膜活性进行了评估。化合物9n9o9q表现出有希望的杀灭K. planticola(MTCC 530)的活性(MIC值为3.9 µg / mL )。它们还显示出对K. planticola的显着杀菌活性(MTCC 530)(MBC值为15.6 µg / mL)。另外,该生物体中9n9o9q抑制生物膜形成(IC 50值在20.28–20.79μg/ mL之间)。

更新日期:2017-10-27
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