Indole-and benzothiophene-based histamine H 3 antagonists

…, D Nepomuceno, MA Letavic, A Lee-Dutra…

Index: Santillan Jr., Alejandro; McClure, Kelly J.; Allison, Brett D.; Lord, Brian; Boggs, Jamin D.; Morton, Kirsten L.; Everson, Anita M.; Nepomuceno, Diane; Letavic, Michael A.; Lee-Dutra, Alice; Lovenberg, Timothy W.; Carruthers, Nicholas I.; Grice, Cheryl A. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 21 p. 6226 - 6230

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Citation Number: 7

Abstract

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. ...