Synthesis of bioactive polyheterocyclic ring systems as 5α-reductase inhibitors

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• 作者：Naglaa A. Abdel Hafez ; Thoraya A. Farghaly ; Mohamed A. Al-Omar ; Mohamed M. Abdalla
• 关键词：Hydrazonoyl halides ; 5α ; -Reductase inhibitors ; Polyheterocycles ; Piperidone
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：November 2010
• 年：2010
• 卷：45
• 期：11
• 页码：4838-4844
• 全文大小：392 K

文摘

Simple synthetic strategies for the hitherto unreported [1,2,4]triazolo[4,3-a]pyrido[4,3-d]pyrimidines 8 and [1,2,4]triazolo[4′,3′:1,2]pyrimido[4,5-b][1,6]naphthyridine-5-one 15 are described based on reaction of thione 3 and 12 with hydrazonoyl chloride 1a–h, respectively. The structures of products 8 and 15 were confirmed by spectroscopic and X-ray crystallographic analyses. Also, the mechanism of such reactions was discussed. In addition, reaction of compound 12 with bromoacetic acid and hydrazine hydrate was investigated. Compounds were screened against 5α-reductase and showed activities with good LD₅₀ and LD₉₀ for all compounds.