6533b86efe1ef96bd12cb684
RESEARCH PRODUCT
Synthesis and in vitro antimicrobial activities of new (cyano-NNO-azoxy) pyrazole derivatives
Stefania AielloGiulia MoraceDonatella BoschiStefano GuglielmoElisa BorghiRoberta Frutterosubject
AzoxyStaphylococcus aureusAntifungal AgentsStereochemistryClinical BiochemistryPharmaceutical ScienceMicrobial Sensitivity TestsPyrazoleBiochemistryChemical synthesisAntifungal activity Pyrazole Azole sistance Cyano-NNO-azoxy Thiophenechemistry.chemical_compoundAnti-Infective AgentsThiopheneCandida kruseiNitrilesDrug DiscoveryThiopheneAntifungal activityIsoxazoleAntifungal activity; Pyrazole; Azole resistance; Cyano-NNO-azoxy; Thiophene.Molecular BiologyCandidaMolecular StructurebiologyCandida glabrataOrganic ChemistryBiological activitybiology.organism_classificationSettore CHIM/08 - Chimica FarmaceuticachemistryCyano-NNO-azoxyPyrazoleAzole resistancePyrazolesMolecular MedicineAzo Compoundsdescription
The antibacterial and antifungal activity of a series of products, in which the 1,5-dimethyl-4-(cyano- NNO-azoxy)pyrazol-3-yl and 1,3-dimethyl-4-(cyano-NNO-azoxy)pyrazol-5-yl moieties were linked to pyridine, pyrazole, isoxazole, thiophene and the furan ring, were examined. No molecule displayed activity against the Gram-negative bacteria tested. Conversely, some compounds displayed activity against two Staphylococcus aureus strains, including the methicillin resistant strain. All compounds displayed interesting antifungal activity, the most active compound of the series being the thiophene derivative 7a. This compound’s activity against Candida krusei and Candida glabrata (MIC = 0.25 and 0.5 lg/mL, respectively), two fungal species resistant to azoles, is noteworthy. The presence of the cyano function appeared essential for activity.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2011-06-01 |