2. Academic Validation
  3. Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists

Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists

  • Bioorg Med Chem Lett. 2010 Nov 15;20(22):6538-41. doi: 10.1016/j.bmcl.2010.09.038.
Zhicai Yang 1,  David J Fairfax,  Jun-Ho Maeng,  Liaqat Masih,  Alexander Usyatinsky,  Carla Hassler,  Soshanna Isaacson,  Kevin Fitzpatrick,  Russell J DeOrazio,  Jianqing Chen,  James P Harding,  Matthew Isherwood,  Svetlana Dobritsa,  Kevin L Christensen,  Jonathan D Wierschke,  Brian I Bliss,  Lisa H Peterson,  Cathy M Beer,  Christopher Cioffi,  Michael Lynch,  W Martin Rennells,  Justin J Richards,  Timothy Rust,  Yuri L Khmelnitsky,  Marlene L Cohen,  David D Manning
Affiliations

Affiliation

  • 1 Discovery R&D AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA.
PMID: 20889341 DOI: 10.1016/j.bmcl.2010.09.038
Abstract

A new class of 2-substituted benzoxazole carboxamides are presented as potent functional 5-HT(3) receptor antagonists. The chemical series possesses nanomolar in vitro activity against human 5-HT(3)A receptors. A chemistry optimization program was conducted and identified 2-aminobenzoxazoles as orally active 5-HT(3) receptor antagonists with good metabolic stability. These novel analogues possess drug-like characteristics and have potential utility for the treatment of diseases attributable to improper 5-HT(3) receptor function, especially diarrhea predominant irritable bowel syndrome (IBS-D).

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