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Syntheses and Biological Activities of Potent Potassium Channel Openers Derived From (+/-)-2-oxo-1-pyridin-3-yl-cyclohexanecarbothioic Acid Methylamide: New Potassium Channel Openers

Syntheses and Biological Activities of Potent Potassium Channel Openers Derived From (+/-)-2-oxo-1-pyridin-3-yl-cyclohexanecarbothioic Acid Methylamide: New Potassium Channel Openers

T J Brown, R F Chapman, J S Mason, M N Palfreyman, N Vicker, R J Walsh

J Med Chem. 1993 May 28;36(11):1604-12.

PMID: 8496928

Abstract:

The syntheses and biological activities of (+/-)-2-(cyanomethylene)-1-pyridin-3-ylcyclohexanecarbothioic++ + acid methylamide (6) and trans-(+/-)-2-(cyanomethyl)-1-pyridin-3-ylcyclohexanecarbothioic acid methylamide (14) derived from (+/-)-2-oxo-1-pyridin-3-ylcyclohexanecarbothioic acid methylamide (4) are reported. Compounds were tested for antagonism of potassium-induced contraction of de-endothelialized rat aorta. The effects of modification of 6 and 14 on in vitro K(+)-channel opening activity are presented. These new series of potassium channel openers so derived are best exemplified by (+/-)-2-[2-(phenylsulfanyl)ethylidene]-1-pyridin-3-ylcyclohexan ecarbothioic acid methylamide (13d, RP 66266) and trans-(+/-)-2-[2-[(phenylsulfonyl)amino]ethyl]-1-pyridin-3- ylcyclohexanecarbothioic acid methylamide (25a, RP 66784), which have IC90 values of 3 and 0.3 nM, respectively. The potency of the most active compounds indicates a possible interaction at an extra binding site. The compounds described herein are potential antihypertensive and antianginal agents.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
LS7931494	Potassium 1-(phenylsulfonyl)-1H-indole-3-trifluoroborate			Price

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