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New P2X3 receptor antagonists. Part 2: Identification and SAR of quinazolinones.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Szántó G,Makó A,Vágó I,Hergert T,Bata I,Farkas B,Kolok S,Vastag M

doi

10.1016/j.bmcl.2016.07.013

subject

Has Abstract

pub_date

2016-08-15 00:00:00

pages

3905-12

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)30715-6

journal_volume

26

pub_type

杂志文章

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