New P2X3 receptor antagonists. Part 2: Identification and SAR of quinazolinones.
Bioorg Med Chem Lett
; 26(16): 3905-12, 2016 08 15.
Article
em En
| MEDLINE
| ID: mdl-27426300
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.
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Base de dados:
MEDLINE
Assunto principal:
4-Quinolonas
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Quinazolinonas
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Receptores Purinérgicos P2X3
/
Antagonistas do Receptor Purinérgico P2X
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article