Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists
ACS Medicinal Chemistry Letters2015Vol. 6(3), pp. 329–333
Citations Over Time
Guy Rouquet, Dianna E. Moore, Malcolm Spain, Daniel M. Allwood, Claudio Battilocchio, David C. Blakemore, Paul V. Fish, Stephen Jenkinson, Alan S. Jessiman, Steven V. Ley, Gordon McMurray, Richard Storer
Abstract
A series of pyrido[3,4-d]azepines that are potent and selective 5-HT2C receptor agonists is disclosed. Compound 7 (PF-04781340) is identified as a suitable lead owing to good 5-HT2C potency, selectivity over 5-HT2B agonism, and in vitro ADME properties commensurate with an orally available and CNS penetrant profile. The synthesis of a novel bicyclic tetrasubstituted pyridine core template is outlined, including rationale to account for the unexpected formation of aminopyridine 13 resulting from an ammonia cascade cyclization.
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