Studies on the Synthesis of Pyrazolyl-thiazolidinedione Derivatives as Antibacterial Agents

• Main Authors: Chong Hou, 鍾浩
• Other Authors: Yeh-Long Chen
• Format: Others
• Language: zh-TW
• Published: 2014
• Online Access: http://ndltd.ncl.edu.tw/handle/wznmup

碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所 === 102 === In recent years, with the evolution of bacteria and abuse of antibiotics, bacteria’s resistance to drugs becomes an important issue in the chemotherapy. Therefore, search for newer and stronger antibiotics are becoming more and more urgent. The present research describes preparation and evaluation of certain potential antibacterial agents by the structural modification of biologically active 1,3-diaryl pyrazole derivatives. We have replaced C-3 aryl group with a versatile quninoline ring, introduced a substituent at C-4 position, and a substituted group on the para position of the C-1 aromatic ring. These compounds were evaluated in vitro against S.aureus and P. acnes. Results indicated that (1) C-4 position prefer to be the 2,4-thiazolidinedione bearing the acid side chain or the rhodanine moiety; (2) C-1 position prefer to be the phenyl ring with a fluoro group substituted at the para position.