A number of heterocycles bearing an arylpiperazinylalkyl side chain and structurally related to the previously described lead ET1 (4-amino-6-methyl-2-[3-(4-p-tolylpiperazin-1-yl)propyl]-5-vinylpyridazin-3 (2H)-one) was synthesized and tested for their antinociceptive activity in Writhing Test. Many compounds, tested at doses of 20–40 mg/kg po were able to reduce the number of abdominal constrictions by more than 47% and, in same cases, the potency is comparable to lead ET1 as for 5e, 24a, 27b and 27c. The analgesia induced by the active compounds was completely prevented by pretreatment with a2-antagonist yohimbine, confirming the involvement of the adrenergic system in the mechanism of action for these new compounds.

Synthesis of five and six-membered heterocycles bearing an arylpiperazinylalkyl side chain as orally active antinociceptive agents / Claudia Vergelli; Giovanna Ciciani; Agostino Cilibrizzi; Letizia Crocetti; Lorenzo Di Cesare Mannelli; Carla Ghelardini; Gabriella Guerrini; Antonella Iacovone; Maria Paola Giovannoni. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - ELETTRONICO. - 23:(2015), pp. 6237-6245.

Synthesis of five and six-membered heterocycles bearing an arylpiperazinylalkyl side chain as orally active antinociceptive agents

VERGELLI, CLAUDIA;CICIANI, GIOVANNA;CROCETTI, LETIZIA;DI CESARE MANNELLI, LORENZO;GHELARDINI, CARLA;GUERRINI, GABRIELLA;IACOVONE, ANTONELLA;GIOVANNONI, MARIA PAOLA
2015

Abstract

A number of heterocycles bearing an arylpiperazinylalkyl side chain and structurally related to the previously described lead ET1 (4-amino-6-methyl-2-[3-(4-p-tolylpiperazin-1-yl)propyl]-5-vinylpyridazin-3 (2H)-one) was synthesized and tested for their antinociceptive activity in Writhing Test. Many compounds, tested at doses of 20–40 mg/kg po were able to reduce the number of abdominal constrictions by more than 47% and, in same cases, the potency is comparable to lead ET1 as for 5e, 24a, 27b and 27c. The analgesia induced by the active compounds was completely prevented by pretreatment with a2-antagonist yohimbine, confirming the involvement of the adrenergic system in the mechanism of action for these new compounds.
2015
23
6237
6245
Goal 3: Good health and well-being for people
Claudia Vergelli; Giovanna Ciciani; Agostino Cilibrizzi; Letizia Crocetti; Lorenzo Di Cesare Mannelli; Carla Ghelardini; Gabriella Guerrini; Antonella...espandi
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1007326
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