| Literature DB >> 27426300 |
Gábor Szántó1, Attila Makó1, István Vágó1, Tamás Hergert1, Imre Bata1, Bence Farkas1, Sándor Kolok1, Mónika Vastag1.
Abstract
Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clinical trials with the most advanced compound. We have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonistic properties. This Letter describes the SAR of a back-up series containing a 4-oxo-quinazoline central ring. The discovery of the highly potent compounds 51 is presented.Entities:
Keywords: 4-Oxo-6-aryl-phenethyl-quinazolines; ATP; Chronic cough; Ion channel; Nanomolar activity; P2X3 antagonist; Purinergic receptor; Structure–activity relationship
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Year: 2016 PMID： 27426300 DOI： 10.1016/j.bmcl.2016.07.013
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823