Design, synthesis, and evaluation of tetrasubstituted pyridines as potent 5-HT2CReceptor agonists

ROUQUET, Guy, MOORE, Dianna E., SPAIN, Malcolm, ALLWOOD, Daniel, BATTILOCCHIO, Claudio, BLAKEMORE, David C., FISH, Paul V., JENKINSON, Stephen, JESSIMAN, Alan S., LEY, Steven V., MCMURRAY, Gordon and STORER, R. Ian (2015). Design, synthesis, and evaluation of tetrasubstituted pyridines as potent 5-HT2CReceptor agonists. ACS Medicinal Chemistry Letters, 6 (3), 329-333.

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Official URL: http://pubs.acs.org/doi/abs/10.1021/ml500507v
Link to published version:: 10.1021/ml500507v

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.

Item Type: Article
Research Institute, Centre or Group: Biomolecular Sciences Research Centre
Identification Number: 10.1021/ml500507v
Depositing User: Marguerite Lyons
Date Deposited: 13 Aug 2015 09:06
Last Modified: 13 Aug 2015 09:06
URI: http://shura.shu.ac.uk/id/eprint/10759

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