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Thiophenecarboxylate suppressor of cyclic nucleotides discovered in a small-molecule screen blocks toxin-induced intestinal fluid secretion.

Lukmanee L Tradtrantip, Buranee B Yangthara, Prashant P Padmawar, Christopher C Morrison, and A S AS Verkman

Mol Pharmacol 75(1):134-42 (2009) PMID 18824527

We carried out a "pathway" screen of 50,000 small molecules to identify novel modulators of cAMP signaling. One class of compounds, the 2-(acylamino)-3-thiophenecarboxylates, strongly suppressed cAMP and cGMP in multiple cell lines in response to different agonists acting on G-protein-coupled receptors, adenylyl cyclase, and guanylyl cyclase. The best compounds from structure-activity analysis of 124 analogs, including several synthesized chiral analogs, had and IC(50) of

DOI: 10.1124/mol.108.050567
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