Indole- and benzothiophene-based histamine H₃ antagonists

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• 作者：Alej ; ro Santillan Jr. ; Kelly J. McClure ; Brett D. Allison ; Brian Lord ; Jamin D. Boggs ; Kirsten L. Morton ; Anita M. Everson ; Diane Nepomuceno ; Michael A. Letavic ; Alice Lee-Dutra ; Timothy W. Lovenberg
• 关键词：Histamine ; Indole ; Benzothiophene ; Mannich reaction ; SAR
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 November 2010
• 年：2010
• 卷：20
• 期：21
• 页码：6226-6230
• 全文大小：903 K

文摘

Previous research on histamine H₃ antagonists has led to the development of a pharmacophore model consisting of a central phenyl core flanked by two alkylamine groups. Recent investigation of the replacement of the central phenyl core with heteroaromatic fragments resulted in the preparation of novel 3,5-, 3,6- and 3,7-substituted indole and 3,5-substituted benzothiophene analogs that demonstrate good to excellent hH₃ affinities. Select analogs were profiled in a rat pharmacokinetic model.