Synthesis of 6-substituted acylpiperazinylphenyl dihydro pyridazinones and their inhibition of platelet aggregation / 第二军医大学学报

ABSTRACT

Objective:To synthesize analogues of 6-[4-(4-substituted acyl piperazinyl)phenyl]-4, 5-dihydro-3(2H)pyri-dazinones and 6-[4-(4-substituted acyl piperazinyl)phenyl]-5-methyl-4,5-dihydro-3(2H)pyridazinones in search for more potent and selective antithrombotic drugs. Methods:Many reactions such as Friedel-Crafts reaction,hydrolysis,cyclation, acyla-tion,substitution were used to synthesize the title compounds. Born method was applied for preliminary pharmacological test in vitro. Results: Twelve title compounds were synthesized, in which 10 compounds were firstly reported. Their structures were identified by element analysis and 1H-NMR. Conclusion:Results of preliminary pharmacological test show that all synthesized compounds are effective against platelet aggregation induced by ADP in vitro. The activity of compound (9) is the most potent. The activity of compound (6), (7), (10), (11), (12) are also better than that of CCI-17810.