145371-35-3Relevant academic research and scientific papers
Synthesis of Mannich bases of arylidenepyridazinones as analgesic agents
Rubat,Coudert,Albuisson,Bastide,Couquelet,Tronche
, p. 1084 - 1087 (2007/10/02)
A series of 5-arylidenepyridazin-3-ones substituted in the 2-position by an arylpiperazinoalkyl moiety (2-16) was synthesized and evaluated for analgesic activity. In the phenylbenzoquinone-induced writhing test, Mannich bases 2-14 were the most active compounds (6.1 ≤ ED50 ≤ 43.0 mg/kg, orally; ED50 is the half-maximal effective dose). Pyridazinones 8 and 9, with a 3-chlorophenylpiperazinomethyl substituent, also exhibited significant anti-inflammatory and antipyretic effects. The activities in the phenylbenzoquinone-induced writhing test were subjected to a Hansch analysis, and a significant correlation with lipophilicity and Hammett's constants was obtained.
