6533b85efe1ef96bd12c05f1
RESEARCH PRODUCT
Antimicrobial and antineoplastic activities of new 4-diazopyrazole derivatives
Benedetta MaggioSalvatore PlesciaMaria Elena MarongiuGiuseppe DaidoneChiara MusiuRaffa DemetrioGraziella PerraC. Miliasubject
PharmacologybiologyChemistryStreptococcusOrganic ChemistryGeneral Medicinemedicine.disease_causebiology.organism_classificationAntimicrobialStreptococcaceaeCorpus albicansMicrobiologyDrug DiscoverymedicineShigellaStaphylococcusBacteriaAntibacterial agentdescription
Abstract Several new 4-diazopyrazole derivatives were prepared by the reaction of 3-methyl-5(substituted-benzamido)pyrazoles with an excess of nitrous acid in acetic acid solution. The compounds were tested for antiretroviral activity in HIV-1 infected MT-4 cells and antiproliferative effects against a panel of human leukemia, lymphoma and solid tumor cell lines. They were also tested for activity against representative gram-negative ( Shigella, Salmonella ) and gram-positive ( S. aureus, D group Streptococcus ) bacteria as well as fungi ( C. albicans, C. paratropicalis, C. neoformans and A. fumigatus ). Compounds were devoid of anti HIV-1 and antimicotic activities, whereas they were active against tumor cell lines, with inhibitory activity (IC 50 ) in the range 2.4–20 μM and bacteria. The highest microbial susceptibility was shown by gram-positive bacteria, with minimum inhibitory concentrations in the range 0.8–12.5 μM.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1998-06-01 | European Journal of Medicinal Chemistry |