Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373525 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
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. Select analogs were profiled in a rat pharmacokinetic model.
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Related Topics
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Authors
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,