6533b821fe1ef96bd127b9c8
RESEARCH PRODUCT
Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
Domenico SchillaciMaria VitaleFabiana PlesciaMaria Valeria RaimondiStella CascioferroGabriella CancemiBenedetta MaggioMaria Grazia CusimanoDemetrio RaffaGiuseppe Daidonesubject
PharmacologyNitrous acidStaphylococcus aureusDose-Response Relationship DrugMolecular StructureStereochemistryOrganic ChemistryBiofilmGeneral MedicineMicrobial Sensitivity Testsmedicine.disease_causeSettore BIO/19 - Microbiologia GeneraleSettore CHIM/08 - Chimica FarmaceuticaAnti-Bacterial Agentschemistry.chemical_compoundStructure-Activity RelationshipchemistryStaphylococcus aureusBiofilmsDrug DiscoverymedicinePyrazolesAcetic acid solution4-diazopyrazoles anti-staphylococcal activity anti-biofilm activityAzo Compoundsdescription
Abstract Several new 4-diazopyrazole derivatives 6a – g and 9a – c were obtained by the reaction of 1-(R-substituted-phenyl)-3-(1,3-dimethyl-1 H -pyrazol-5-yl)ureas 5a – g and N -(1,3-dimethyl-1 H -pyrazol-5-yl)-2-(R-substituted-phenyl)acetamides 8a – c respectively with a sevenfold excess of nitrous acid in acetic acid solution. The compounds were assayed for their activity against the Staphylococcus aureus reference strains ATCC 25923, ATCC 29213 and ATCC 6538, as well as six veterinary strains. The best anti-staphylococcal profile was showed by [(R-substituted-phenyl)acetyl](4-diazonio-1,3-dimethyl-1 H -pyrazol-5-yl)azanides 9a , c . Compound 9c was also able at 3.1 μg mL −1 to inhibit of 45.7% the biofilm formation of the strains S. aureus ATCC 29213.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2012-08-10 | European journal of medicinal chemistry |