title: Synthesis and anti-infective evaluation of 5-amino-N-phenylpyrazine-2-carboxamides.
abstract: A series of eleven novel 5-amino-N-phenylpyrazine-2-carboxamides were synthesized and evaluated for in vitro anti-infective properties. Prepared compounds were characterized by IR, 1H NMR and 13C NMR spectra, elementary analysis and melting points. Lipophilicity parameters Log P and ClogP were calculated. None of the compounds was effective against any of tested mycobacterial strains (Mycobacterium tuberculosis H37Rv, M. kansasii, M. avium) up to concentration of 100 μg/mL. 5-amino-N-(2,5-dimethylphenyl) pyrazine-2-carboxamide (3) exerted moderate antibacterial activity against Staphylococcus aureus (MIC = 62.5 μM). No antifungal activity was detected. Several compounds exerted moderate antiviral activity against influenza A viruses at the level of tens of μM.Key words: pyrazinamide antimycobacterial activity antibacterial activity antifungal activity antiviral activity.
authors.forename: Jan
authors.initials: J
authors.lastname: Zitko
authors.forename: Fernando
authors.initials: F
authors.lastname: Franco
authors.forename: Pavla
authors.initials: P
authors.lastname: Paterová
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D011718:Pyrazinamide / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; D011718:Pyrazinamide