Indole- and benzothiophene-based histamine H3 antagonists

✍ Scribed by Alejandro 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; Nicholas I. Carruthers; Cheryl A. Grice

• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 904 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.08.103

✦ Synopsis

Previous research on histamine H 3 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 hH 3 affinities. Select analogs were profiled in a rat pharmacokinetic model.