吡唑噻唑二酮衍生物作為抗菌試劑之研究與合成

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

鍾浩(Chong Hou)

指導教授 ： 陳義龍

高雄醫學大學/生命科學院/醫藥暨應用化學研究所/碩士(2014年)

https://doi.org/10.6832/KMU.2014.00097

摘要

近年來，隨著細菌的突變以及抗生素濫用的關係，陸續出現更多具有抗藥性的細菌，所以必需尋找更新更強的抗菌藥物以供人類需要。在文獻中發現1,3 - 二芳基吡唑衍生物具有抗菌等多種生物活性，本研究論文主要是探討改變吡唑1號位置上芳香環的取代基，在3號位置換成具有多種生物活性的喹啉基團，並且在4號位置上接若單寧等不同的結構來得到一系列新型抗菌的化合物。這些化合物在抑制金黃色葡萄球菌(S. aureus ATCC 29213)以及痤瘡桿菌(P. acnes BCRC10723)的活性測試中，我們發現到在吡唑基1號位置為4-氟苯取代，且4號位置上接上有酸取代的噻唑烷二酮或若單寧衍生物具有良好的抗菌活性。

關鍵字

吡唑噻唑二酮衍生物

並列摘要

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.

並列關鍵字

Pyrazolyl-thiazolidinedione Derivatives

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