852180-52-0Relevant articles and documents
Indole- and benzothiophene-based histamine H3 antagonists
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.
scheme or table, p. 6226 - 6230 (2010/12/18)
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.