Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action

…, C Ghelardini, N Galeotti, MP Giovannoni

Index: Cesari, Nicoletta; Biancalani, Claudio; Vergelli, Claudia; Dal Piaz, Vittorio; Graziano, Alessia; Biagini, Pierfrancesco; Ghelardini, Carla; Galeotti, Nicoletta; Giovannoni, Maria Paola Journal of Medicinal Chemistry, 2006 , vol. 49, # 26 p. 7826 - 7835

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Citation Number: 32

Abstract

A number of arylpiperazinylalkylpyridazinones structurally related to the previously described lead A (5-{[4-(3-chlorophenyl) piperazin-1-yl]-propyl}-3-methyl-7- phenylisossazolo [4, 5-d] pyridazin-4-(5 H)-one) were synthesized and tested for their analgesic activity. Many of the tested molecules, at the dose of 20 mg kg-1 po, showed high antinociceptive activity, in particular, compounds 5a, 11c, 15a, 21 and 22, which were able ...