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

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

  • Bioorg Med Chem Lett. 2010 Dec 1;20(23):7155-8. doi: 10.1016/j.bmcl.2010.07.053.
Jane L Wang 1,  Jeffery Carter,  James R Kiefer,  Ravi G Kurumbail,  Jennifer L Pawlitz,  David Brown,  Susan J Hartmann,  Matthew J Graneto,  Karen Seibert,  John J Talley
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Chesterfield, MO 63017, USA. jl47wang@yahoo.com
PMID: 21055613 DOI: 10.1016/j.bmcl.2010.07.053
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.

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