2. Academic Validation
  3. Optimization of sulfonamide derivatives as highly selective EP1 receptor antagonists

Optimization of sulfonamide derivatives as highly selective EP1 receptor antagonists

  • Bioorg Med Chem. 2006 Dec 1;14(23):7774-89. doi: 10.1016/j.bmc.2006.08.001.
Atsushi Naganawa 1,  Toshiaki Matsui,  Masaki Ima,  Koji Yoshida,  Hiroshi Tsuruta,  Shingo Yamamoto,  Hiroshi Yamamoto,  Hiroki Okada,  Takayuki Maruyama,  Hisao Nakai,  Kigen Kondo,  Masaaki Toda
Affiliations

Affiliation

  • 1 Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka 618-8585, Japan. naganawa@ono.co.jp
PMID: 16931028 DOI: 10.1016/j.bmc.2006.08.001
Abstract

A series of 4-[(2-{isobutyl[(5-methyl-2-furyl)sulfonyl]amino}phenoxy)methyl]benzoic acids and 4-({2-[isobutyl(1,3-thiazol-2-ylsulfonyl)amino]phenoxy}methyl)benzoic acids were synthesized and evaluated for their EP receptor affinities and EP1 receptor antagonist activities. Further structural optimization was carried out to reduce inhibitory activity against hepatic Cytochrome P450 isozymes, which could represent a harmful potential drug interaction. Selected compounds were also evaluated for their binding affinities to hTP, hDP, mFP, and hIP, and for their hEP1 receptor antagonist activities. The results of structure-activity relationship studies are also presented.

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