Novel substituted quinoxaline 1,4-dioxides with in vitro antimycobacterial and anticandida activity.
Thirty-six 6(7)-substituted-3-methyl- or 3-halogenomethyl-2-phenylthio-phenylsulphonyl-chloro-quinoxaline 1,4-dioxides belonging to series 3-6 were synthesised and submitted to a preliminary in vitro evaluation for antimycobacterial, anticandida and antibacterial activities. Antitubercular screening showed a generally good activity of 3-methyl-2-phenylthioquinoxaline 1,4-dioxides (3d,e,h-j) against Mycobacterium tuberculosis, and exhibited MIC between 0.39 and 0.78 microg mL(-1) (rifampicin MIC=0.25 microg mL(-1)), whereas in compounds 4d,e, 5a,b,d,e,l and 6b-e,j,l MIC ranged between 1.56 and 6.25 microg mL(-1). Results of the antibacterial and anticandida screening showed that 6e and 6l exhibited MIC=0.4 and 1.9 microg mL(-1), respectively, against Candida krusei (miconazole MIC=0.9 microg mL(-1)), and 4i, 5b,d, 6e, MIC=3.9 microg mL(-1) against Candida glabrata (miconazole MIC=0.4 microg mL(-1)), while compounds 3d,l, 5e,l, and 6b,d,e,l showed MIC=15.6 microg mL(-1) against Vibrio alginolyticus.
Carta
Antonio
A
Dipartimento Farmaco Chimico Tossicologico, via Muroni 23/a, 07100 Sassari, Italy.
Paglietti
Giuseppe
G
Rahbar Nikookar
Mohammad E
ME
Sanna
Paolo
P
Sechi
Leonardo
L
Zanetti
Stefania
S
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002175:Candida / Q000187:drug effects*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D000995:Antitubercular Agents; D011810:Quinoxalines; C003282:quindoxin