1.
Bioorg Med Chem Lett
; 27(4): 1109-1114, 2017 02 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-28111141
RESUMO
A spirocyclic class of ROMK inhibitors was developed containing a structurally diverse heterocyclic sulfone moiety and spirocyclic core starting from lead 1. These compounds not only displayed exquisite ROMK potency but significantly improved selectivity over hERG. The lead compounds were found to have favorable pharmacokinetic properties and displayed robust diuretic, natriuretic and blood pressure lowering effects in spontaneously hypertensive rats.