Antimicrobial and antineoplastic activities of new 4-diazopyrazole derivatives

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.