Some pyrrole substituted aryl pyridazinone and phthalazinone derivatives and their antihypertensive activities

• Published in: European journal of medicinal chemistry Vol. 39; no. 12; pp. 1089 - 1095
• Main Authors: Demirayak, Seref, Karaburun, Ahmet Cagri, Beis, Rana
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Masson SAS 01-12-2004; Elsevier
• Subjects: Animals; Antihypertensive activity; Antihypertensive agents; Antihypertensive Agents - chemical synthesis; Antihypertensive Agents - pharmacology; Aorta - drug effects; Biological and medical sciences; Cardiovascular system; In Vitro Techniques; Male; Medical sciences; Molecular Structure; Pharmacology. Drug treatments; Phthalazines - chemical synthesis; Phthalazines - pharmacology; Phthalazinone; Pyridazines - chemical synthesis; Pyridazines - pharmacology; Pyridazinone; Pyrrole; Pyrroles - chemical synthesis; Pyrroles - pharmacology; Rats; Rats, Wistar; Vasodilation - drug effects; Phthalazinone; Antihypertensive activity; Pyridazinone; Pyrrole; Five membered ring; Rat; Nitrogen heterocycle; Rodentia; Benzene derivatives; In vitro; Pyrrole derivatives; Phthalazine derivatives; In vivo; Vertebrata; Mammalia; Structure activity relation; Animal; Six membered ring; Bicyclic compound; Antihypertensive agent; Pyridazine derivatives; Aromatic compound; Chemical synthesis
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2004.09.005

In this work, some 2-nonsubstituted/2-methyl-/2-(2-acetyloxyethyl)-6-[4-(substituted pyrrol-1-yl)phenyl]-4,5-dihydro-3(2H)-pyridazinone, derivatives and 2-nonsubstituted/2-methyl- 4-[4-(substituted pyrrol-1-yl)phenyl]-1(2H)-phthalazinone derivatives were synthesised by reacting hexan-2,5-dion or 1-aryl-3-carbethoxypent-1,4-diones with corresponding 2-substituted/nonsubstituted 6-(4’-aminophenyl)-4,5-dihydro-3(2H)-pyridazinone or 2-substituted/nonsubstituted-4-(4’-aminophenyl)-(2H)-phthalazinone under Paal–Knorr pyrrole synthesis conditions. The antihypertensive activities of the compounds were examined both in vitro and in vivo. Some pyridazinone derivatives showed appreciable activity.