Synthesis and evaluation for biological activity of 3-alkyl and 3-halogenoalkyl-quinoxalin-2-ones variously substituted. Part 4.
A new series of 3-isopropyl-, 3-trifluoromethyl- and 3-bromomethylquinoxaline-2-ones variously substituted on the benzo-moiety were synthesized and submitted to a preliminary in vitro evaluation for antibacterial, antifungal and anti-HIV activities. Furthermore, all compounds were also tested for cytotoxicity. Results of the screening showed that compound 10 exhibits moderate antimicrobial activity against Staphylococcus aureus (MIC = 33 microM), and that 25 and 26 showed interesting cytotoxicity versus mock-infected MT-4 cells. All the other compounds were inactive.
Carta
Antonio
A
Dipartimento Farmaco Chimico Tossicologico, Universitá di Sassari, Italy.
Sanna
Paolo
P
Loriga
Mario
M
Setzu
Maria Giovanna
MG
La
Colla Paolo
CP
Loddo
Roberta
R
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006678:HIV / Q000187:drug effects; D006801:Humans; D016014:Linear Models; D008826:Microbial Sensitivity Tests; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000890:Anti-Infective Agents; D000935:Antifungal Agents; D000998:Antiviral Agents; D011810:Quinoxalines