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ID: ALA1287761

Journal: Bioorg Med Chem Lett

Title: The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: the first clinical candidate.

Authors: Wang JL, Carter J, Kiefer JR, Kurumbail RG, Pawlitz JL, Brown D, Hartmann SJ, Graneto MJ, Seibert K, Talley JJ.

Abstract: In this manuscript, we report the discovery of the substituted 2-trifluoromethyl-2H-benzopyran-3-carboxylic acids as a novel series of potent and selective cyclooxygenase-2 (COX-2) inhibitors. 5c-(S) (SD-8381) was advanced into clinical studies due to its superior in vivo potency. The high plasma protein binding (>99% bound) of 5c-(S) has resulted in a surprisingly long human half life t(1/2)=360 h.

CiteXplore: 21055613

DOI: 10.1016/j.bmcl.2010.07.053