Bouherrou Houria, Saidoun Aicha, Abderrahmani Ahmed, Abdellaziz Lamia, Rachedi Yahia, Dumas Françoise, Demenceau Albert
Laboratory of Applied Organic Chemistry, Faculty of Chemistry, University of Science and Technology Houari Boumediene, BP 32, El Alia, 16111 Bab Ezzouar, Algiers, Algeria.
Laboratory of Cellular and Molecular Biology, Faculty of Biological Sciences, USTHB, BP 32, El Alia, 16111 Bab Ezzouar, Algiers, Algeria.
Molecules. 2017 May 7;22(5):757. doi: 10.3390/molecules22050757.
An efficient and green method has been developed for the synthesis of new substituted Hantzsch thiazole derivatives in 79%-90% yield, via the one-pot multi-component procedure, by the reaction of 3-(bromoacetyl)-4-hydroxy-6-methyl-2-pyran-2-one, thiourea and substituted benzaldehydes in the presence of silica supported tungstosilisic acid, as a reusable catalyst, under conventional heating or under ultrasonic irradiation. The catalyst is recoverable by a simple filtration and can be reused in the subsequent reactions. Most of the thiazoles exhibited significant antibacterial activity compared toamoxicillin and ciprofloxacin as positive controls. In addition, the new compounds showed moderate to good antioxidant (DPPH) radical scavenging activity.
已经开发出一种高效、绿色的方法,通过一锅多组分反应,在硅胶负载的钨硅酸作为可重复使用催化剂的存在下,于常规加热或超声辐射条件下,使3-(溴乙酰基)-4-羟基-6-甲基-2-吡喃-2-酮、硫脲和取代苯甲醛反应,以79%-90%的产率合成新的取代汉茨希噻唑衍生物。该催化剂可通过简单过滤回收,并可在后续反应中重复使用。与作为阳性对照的阿莫西林和环丙沙星相比,大多数噻唑表现出显著的抗菌活性。此外,新化合物还表现出中度至良好的抗氧化(DPPH)自由基清除活性。