ACETYLCHOLINESTERASE INHIBITION ACTIVITY OF SOME QUINOLINYL SUBSTITUTED TRIAZOLOTHIADIAZOLE DERIVATIVES.

Muhammad Rafiq, Qamar Abbas, Muhammad Saleem, Muhammad Hanif, Ki Hwan Lee, Sung-Yum Seo
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Abstract

A series of aralkanoic acids was converted into aralkanoic acid hydrazides through their esters formation. The aralkanoic acid hydrazides upon treatment with carbon disulfide and methanolic potassium hydroxide yielded potassium dithiocarbazinate salts, which on refluxing with aqueous hydrazine hydrate yielded 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles. The target compounds, 3-aralkyl-6-(substitutedquinolinyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, were synthesized by condensing various quinolinyl substituted carboxylic acids with 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles in phosphorus oxychloride. The structures of the newly synthesized triazolothiadiazoles were characterized by IR, 1H NMR, 13C NMR, and elemental analysis studies. The structure of one of the 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles was unambiguously deduced by single crystal X-ray diffraction analysis. All the synthesized compounds were screened for their acetylcholinesterase inhibition activities. Four of the triazolothiadiazoles exhibited excellent acetylcholinesterase inhibition activities as compared to the reference inhibitor.

喹啉基取代三唑噻二唑衍生物的乙酰胆碱酯酶抑制活性。
一系列的烷烃酸通过酯的形成转化为烷烃酸酰肼。用二硫化碳和甲醇氢氧化钾处理后得到二硫代氨基甲酸钾盐,用水合肼回流得到5-芳烷基-4-氨基-3-巯基-1,2,4-三唑。以不同的喹啉基取代羧酸与5-芳烷基-4-氨基-3-巯基-1,2,4-三唑在氯氧磷中缩合,合成了目标化合物3-芳烷基-6-(取代喹啉基)[1,2,4]三唑[3,4-b][1,3,4]噻二唑。通过IR、1H NMR、13C NMR和元素分析对新合成的三唑噻唑进行了结构表征。通过单晶x射线衍射分析,确定了其中一种5-芳烷基-4-氨基-3-巯基-1,2,4-三唑的结构。对合成的化合物进行了乙酰胆碱酯酶抑制活性的筛选。与参比抑制剂相比,四种三唑噻唑类抑制剂表现出良好的乙酰胆碱酯酶抑制活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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