Synthesis of 6-substituted acylpiperazinylphenyl dihydro pyridazinones and their inhibition of platelet aggregation
- VernacularTitle:6-取代乙酰哌嗪苯基二氢哒嗪酮类化合物的合成及其抑制血小板聚集的作用
- Author:
Dongming ZHAO
;
Chaomei LIU
- Publication Type:Journal Article
- Keywords:
synthesis;
pyridazinones;
platelet aggregation inhibitiors
- From:
Academic Journal of Second Military Medical University
1985;0(05):-
- CountryChina
- Language:Chinese
-
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.
