Design and Synthesis of Novel Potent Antinociceptive Agents: Methyl-imidazolyl N-Acylhydrazone Derivatives

This paper describes recent results of design, synthesis and pharmacological evaluation of new N-heterocyclic functionalized N-acylhydrazone compounds, belonging to the 2-methyl-imidazolyl-3-acylhydrazone class ( 4a– e). These compounds were planned by applying the molecular simplification strategy...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2000-09, Vol.8 (9), p.2243-2248
Main Authors: Figueiredo, Juliana M, Câmara, Celso de A, Amarante, Emanuel G, Miranda, Ana Luisa P, Santos, Fúlvia M, Rodrigues, Carlos R, Fraga, Carlos Alberto M, Barreiro, Eliezer J
Format: Article
Language:English
Subjects:
Acetic Acid
Analgesics
Analgesics - chemical synthesis
Analgesics - pharmacology
Animals
Biological and medical sciences
Carrageenan
Colic - chemically induced
Colic - drug therapy
Colic - prevention & control
Drug Design
Edema - chemically induced
Edema - drug therapy
Edema - prevention & control
Female
Heterocyclic Compounds - chemistry
Heterocyclic Compounds - pharmacology
Hydrazones - chemical synthesis
Hydrazones - chemistry
Hydrazones - pharmacology
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - pharmacology
Male
Medical sciences
Mice
Models, Animal
Neuropharmacology
Pharmacology. Drug treatments
Rats
Structure-Activity Relationship
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Summary:This paper describes recent results of design, synthesis and pharmacological evaluation of new N-heterocyclic functionalized N-acylhydrazone compounds, belonging to the 2-methyl-imidazolyl-3-acylhydrazone class ( 4a– e). These compounds were planned by applying the molecular simplification strategy to propose the structural modifications on the previously described functionalized imidazo[1,2- a]pyridine 3-acylhydrazone series ( 2), which presented an important analgesic profile. This new series ( 4) was synthesized in order to investigate the possible pharmacophoric contribution of the N-heteroaromatic ring and N-acylhydrazone moieties to the analgesic activity. Compounds 4a– b are the most potent antinociceptive agents from this series.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(00)00152-8