95355-15-0Relevant academic research and scientific papers
Conformationally Restricted Congeners of Hypotensive and Platelet Aggregation Inhibitors: 6-Aryl-5-methyl-4,5-dihydro-3(2H)-pyridazinones Derived from 5H-Indenopyridazine
Cignarella, Giorgio,Barlocco, Daniela,Pinna, Gerard A.,Loriga, Mario,Tofanetti, Odoardo,et al.
, p. 2191 - 2194 (1986)
A number of 7-amino and 7-acylamino substituted 4,4a-dihydro-5H-indenopyridazin-3-ones have been synthesized as rigid congeners of hypotensive 6-aryl-5-methyl-4,5-dihydro-3(2H)-pyridazinones and tested as antihypertensive, antithrombotic, antiulcer, and antiinflammatory agents.Unlike the previously described 7-cyano derivative, which displayed only antiinflammatory action, the new series exhibited significant antihypertensive and antithrombotic properties.In this respect, the 7-amino (2b) and the 7-acetylamino (2c) derivatives were found to be the most potentand long lasting in reducing the blood pressure in spontaneously hypertensive rats and in protecting mice from the induction of thrombosis.These compounds, as well as the 7-(2-chloropropionyl) derivative 2d, also exhibited antiinflammatory activity; in addition, 2c,d were highly effective in inhibiting indomethacin-induced ulcers in the rat.
Studies on agents with vasodilator and β-blocking activities. V. Synthesis and pharmacological activity of the optical isomers of TZC-5665
Seki, Toshimi,Kanada, Arihiro,Nakao, Tomio,Shiraiwa, Masahumi,Asano, Hajime,Miyazawa, Katuhiko,Ishimori, Tsutomu,Minami, Nobuyoshi,Shibata, Kenyu,Yasuda, Kikuo
, p. 84 - 96 (2007/10/03)
Synthesis of the four optical isomers of TZC-5665 (1), a candidate for the treatment of congestive heart failure, was achieved by the reaction of chiral diaminopyridazinone (2) with chiral glycidyl ether (3). The hypotensive and β-blocking activities of 1 and its optical isomers were examined when given intravenously into anesthetized rats. Furthermore these compounds were evaluated for inhibitory activity on cAMP phosphodiesterase III. Among the four optical isomers, R(A),S(B)-one (1c) possessed the essential activities of TZC-5665 (1).
