Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.
Bioorg Med Chem Lett
; 29(5): 688-693, 2019 03 01.
Article
em En
| MEDLINE
| ID: mdl-30728111
ABSTRACT
Some P2X3 receptor antagonists have been developed as new therapeutic drugs for pain. We discovered a novel chemotype of P2X3 receptor antagonists with a pyrrolinone skeleton. Because of SAR studies to improve bioavailability of lead compound 2, compound (R)-24 was identified, which showed an analgesic effect against neuropathic pain by oral administration. We constructed a human P2X3 homology model as a template for the zebrafish P2X4 receptor, which agreed with SAR studies of pyrrolinone derivatives.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Receptores Purinérgicos P2X3
/
Antagonistas do Receptor Purinérgico P2X
Limite:
Humans
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article