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Updated: Jun 8, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists
Zhicai Yang1, David J Fairfax, Jun-Ho Maeng
1Discovery R&D AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA.
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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