Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity

  • Bioorg Med Chem Lett. 1999 Sep 20;9(18):2773-8. doi: 10.1016/s0960-894x(99)00461-8.
R J Chambers  1 ,  A Marfat ,  G W Antognoli ,  J B Cheng ,  D B Damon ,  A V Kuperman ,  T C Liston ,  C Mebus ,  J S Pillar ,  J T Shirley ,  J W Watson
Affiliations
  • 1. Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
PMID: 10509933 DOI: 10.1016/s0960-894x(99)00461-8
Abstract

CP-199,330 (3) and CP-199,331 (4) are cysLT1 receptor antagonists that are equipotent to marketed cysLT1 receptor antagonists zafirlukast and pranlukast, show good pharmacokinetics in rats and monkeys, and are devoid of liver toxicity in monkeys as seen in CP-85,958 (1).

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