Article

4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action.

Dipartimento di Scienze Farmaceutiche, via Ugo Schiff 6, Sesto Fiorentino, 50019 Firenze, Italy.
Bioorganic & Medicinal Chemistry (impact factor: 2.92). 09/2007; 15(16):5563-75. DOI:10.1016/j.bmc.2007.05.035 pp.5563-75
Source: PubMed

ABSTRACT A series of 4-amino-5-vinyl-3(2H)-pyridazinones and analogues were synthesized and their antinociceptive effect was evaluated in the mouse abdominal constriction model. Several of the novel compounds showed ED(50) values in the range 6-20mg/kg/sc and demonstrated to be able to completely protect all the treated animals from the effect of the noxious stimulus at 30 mg/kg/sc. SAR studies confirmed the essential role played by an amino or substituted amino function at position 4 and by a vinyl group at position 5 of the diazine system.

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Keywords

4-amino-5-vinyl-3(2H)-pyridazinones
 
amino
 
amino function
 
analogues
 
mouse abdominal constriction model
 
novel compounds
 
noxious stimulus
 
position 4
 
position 5
 
SAR studies
 
vinyl group