Novel Steroidal （6R）-Spiro-1,3,4-thiadiazoline Derivatives as Anti-bacterial Agents

作     者：Khan Salman A. Asiri, Abdullah M. 

作者机构：Chemistry Department Faculty of Science King Abdulaziz University P.O. Box 80203 Jeddah 21589 Saudi Arabia Center of Excellence for Advanced Materials Research King Abdulaziz University Jeddah 21589 P.O. Box 80203 Saudi Arabia 

出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)

年 卷 期：2012年第30卷第8期

页      面：1901-1905页

核心收录：

学科分类：080503[工学-材料加工工程] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0805[工学-材料科学与工程（可授工学、理学学位）] 0703[理学-化学] 

主　　题：steroidal thiosemicarbazones steroidal thiadiazolines cholesterol amoxicillin antibacterial activity 

摘      要：Novel steroidal （6R）-spiro-1,3,4-thiadiazoline derivatives have been synthesized by the cyclization of steroidal thiosemiearbazones. Thiosemicarbazones have been synthesized by the reaction of steroidal ketones with thiosemi- carbazide. All the compounds have been characterized by IR, 1H NMR, mass and elemental analyses. The antibacterial activities of these compounds have been first tested in vitro by the disk diffusion assay against two Gram-positive and two Gram-negative bacteria, and then the minimum inhibitory concentration （MIC） values have been determined with the reference of standard drug amoxicillin. The results showed that steroidal thiadiazoline de- rivatives exhibited better antibacterial activity than the steroidal thiosemicarbazone derivatives. Chloro and acetoxy substituents on the 3β-position of the steroidal thiadiazoline ring increased the anti-bacterial activity. Among all the compounds, compounds 7 and 8 were found better inhibitors as compared to the respective drug amoxicillin.