Design,Synthesis,and Hypnotic Activi

Design,Synthesis,and Hypnotic Activity of Pyrazolo[1,5-a]pyrimidine Derivatives

On the basis of the Zaleplon structure, novel pyrazolo[1,5-a]pyrimidines were designed and prepared for studies on their hypnotic activity.This paper reported the synthesis of twelve new 5-methyl-7-substituted-pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives by using simple starting materials such as propane dinitrile and triethyl orthoformate.The structures of the derived target compounds were confirmed by their IR and 1H-NMR spectroscopic data.The preliminary pharmacological evaluations indicated that some compounds showed hypnotic activity, while derivative 1c was the most potent one.

作 者： Song Qing WANG Lin FANG Xiu Jie LIU Kang Zhao   作者单位： Song Qing WANG,Lin FANG,Xiu Jie LIU(College of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016)

Kang Zhao(College of Pharmaceuticals and Biotechnology, Tianjin University, Tianjin 300072) 

刊 名： 中国化学快报(英文版)  ISTIC SCI 英文刊名： CHINESE CHEMICAL LETTERS  年，卷(期)： 2004 15(8)  分类号：   关键词： GABA,hypnotic drug,synthesis,pyrazolo[1,5-a]pyrimidines  

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