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Discovery of a novel sub-class of ROMK channel inhibitors typified by 5-(2-(4-(2-(4-(1H-Tetrazol-1-yl)phenyl)acetyl)piperazin-1-yl)ethyl)isobenzofuran-1(3H)-one.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Nov 01; Vol. 23 (21), pp. 5829-32. Date of Electronic Publication: 2013 Sep 06. - Publication Year :
- 2013
-
Abstract
- A sub-class of distinct small molecule ROMK inhibitors were developed from the original lead 1. Medicinal chemistry endeavors led to novel ROMK inhibitors with good ROMK functional potency and improved hERG selectivity. Two of the described ROMK inhibitors were characterized for the first in vivo proof-of-concept biology studies, and results from an acute rat diuresis model confirmed the hypothesis that ROMK inhibitors represent new mechanism diuretic and natriuretic agents.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Benzofurans pharmacokinetics
Diuresis drug effects
Drug Discovery
Ether-A-Go-Go Potassium Channels antagonists & inhibitors
Ether-A-Go-Go Potassium Channels metabolism
Humans
Potassium Channels, Inwardly Rectifying metabolism
Rats
Rats, Sprague-Dawley
Tetrazoles chemistry
Tetrazoles pharmacokinetics
Tetrazoles pharmacology
Benzofurans chemistry
Benzofurans pharmacology
Potassium Channels, Inwardly Rectifying antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 23
- Issue :
- 21
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24075732
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.08.104