The synthesis of novel pyridazinone derivatives and investigation of their biological properties have gained more importance in recent decades. In particular, the pharmacological activity of 4,5-dihydro-6-phenyl-3(2H)-pyridazinones has been extensively studied and such substances are known for their cardiovascular effects. In this field, several compounds such as zardaverine or imazodan have been developed as PDE III inhibitors in the search for new antiplatelet or cardiotonic agents. A number of 6-aryl-2-(4-aryl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)-4,5-dihydropyridazin-3(2H)-ones have been designed and synthesized by a sequence of reactions starting from the respective aryl hydrocarbons. The final products (4a–4u) were evaluated for their antihypertensive activity by a non-invasive protocol using the tail-cuff method. Compounds 4e, 4i, and 4k showed appreciable properties comparable with that of hydralazine and propranolol.
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Triazolylpyridazinones as a New Class of Antihypertensive Agents: Design, Synthesis and In vivo Screening
Published: 07 November 2016 by MDPI in 2nd International Electronic Conference on Medicinal Chemistry session ECMC-2
Keywords: Pyridazinone, 1,2,4-Triazole, Antihypertensive activity, Non-invasive method