Design and synthesis of a series of combined vasodilator-. beta.-adrenoceptor antagonists based on 6-arylpyridazinones

RA Slater, W Howson, GTG Swayne…

Index: Slater; Howson; Swayne; Taylor; Reavill Journal of Medicinal Chemistry, 1988 , vol. 31, # 2 p. 345 - 351

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Citation Number: 26

Abstract

A series of new 6-[4-[[(aryloxy) acyl] amino] phenyl]-4, 5-dihydropyridazinones have been synthesized and evaluated as combined vasodilator/@-adrenoceptor antagonists and potential antihypertensive agents. Many of the early compounds displayed an unacceptably high level of intrinsic sympathomimetic activity (ISA) and a relatively short duration of action. Disubstitution in the 2, 3-positions or in the 4-position of the aryloxy ring gave compounds ...