期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 21, 页码 5829-5832出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.08.104
关键词
ROMK; Hypertension; Heart failure; Diuresis; Natriuresis
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. (C) 2013 Elsevier Ltd. All rights reserved.
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