Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2014 Jun 20

PMID 24944750

Citations 5

Authors

Harry R Chobanian

Yan Guo

Ping Liu

Marc D Chioda

Selena Fung

Thomas J Lanza

Linda Chang

Raman K Bakshi

James P Dellureficio

Qingmei Hong

Mark McLaughlin

Kevin M Belyk

Shane W Krska

Amanda K Makarewicz

Elliot J Martel

Joseph F Leone

Lisa Frey

Bindhu Karanam

Maria Madeira

Raul Alvaro

Joyce Shuman

Gino Salituro

Jenna L Terebetski

Nina Jochnowitz

Shruti Mistry

Erin McGowan

Richard Hajdu

Mark Rosenbach

Catherine Abbadie

Jessica P Alexander

Lin-Lin Shiao

Kathleen M Sullivan

Ravi P Nargund

Matthew J Wyvratt

Linus S Lin

Robert J DeVita

Affiliations

Soon will be listed here.

Abstract

We report herein the identification of MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal chemistry efforts focused on optimizing of FAAH inhibition in vitro potency, improving the pharmacokinetic (PK) profile, and increasing in vivo efficacy in rodent inflammatory and neuropathic pain assays.

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