Synthesis, structure and antibacterial evaluation of some N-substituted 3-amino-5-hydroxy-4-phenyl-1H-pyrazole-1-carboxamides.

doi:10.2174/157340611797928433

Paper

Synthesis, structure and antibacterial evaluation of some N-substituted 3-amino-5-hydroxy-4-phenyl-1H-pyrazole-1-carboxamides.

Published Oct 31, 2011 · M. Pitucha, U. Kosikowska, Liliana Urszula

Medicinal chemistry (Shariqah (United Arab Emirates))

Q3 SJR score

11

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0

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Abstract

N-substituted 3-amino-5-hydroxy-4-phenyl-1H-pyrazole-1-carboxamide derivatives have been prepared by heterocyclization of 1-cyanophenyl acetic acid hydrazide with isocyanates. Representative compounds were evaluated as potential antimicrobial agents. The most promising compound in this series, the N-(1-naphthyl)-3-amino-5-hydroxy-4-phenyl-1H-pyrazole-1-carboxamide 2f, was the most effective against the reference strains of pathogenic S. aureus ATCC 25923 and S. aureus ATCC 6538 or opportunistic S. epidermidis ATCC 12228 with MIC value of 7.81 μg/ml and against the other gram-positive species with MIC values 15.63-31.25 μg/ml. This compound also showed high activity against clinical isolates of MSSA (methicillin-sensitive Staphylococcus aureus) with MIC of 0.98-31.25 μg/ml and MRSA (methicillin-resistant Staphylococcus aureus) with MIC of 1.96-7.81 μg/ml.

In Vitro Study

Study Snapshot

N-(1-naphthyl)-3-amino-5-hydroxy-4-phenyl-1H-pyrazole-1-carboxamide 2f shows promising antibacterial activity against pathogenic and opportunistic bacteria, with high activity against MSSA and MRSA clinical isolates.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Synthesis, structure and antibacterial evaluation of some N-substituted 3-amino-5-hydroxy-4-phenyl-1H-pyrazole-1-carboxamides.

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