Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema.
ACS Med Chem Lett
; 4(2): 293-6, 2013 Feb 14.
Article
em En
| MEDLINE
| ID: mdl-24900661
ABSTRACT
High-throughput screening and subsequent hit optimization identified 1-piperidinylbenzimidazoles, exemplified by compound 1, as TRPV4 inhibitors. Lead optimization identified potent TRPV4 blocker 19, which has good target activity and pharmacokinetic properties. Inhibitor 19 was then profiled in an in vivo rat model, demonstrating its ability to inhibit TRPV4-mediated pulmonary edema.
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Base de dados:
MEDLINE
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article