In vitro and in vivo activities of HQQ-3, a new triazole antifungal agent.
The activity of HQQ-3, a new triazole antifungal agent, was evaluated and compared with those of fluconazole, ketoconazole and terbinafine in vitro and with fluconazole in vivo. HQQ-3 exhibited potent in vitro activity against clinically important fungi. The activity of HQQ-3 against Candida spp. was superior to those of fluconazole and terbinafine and comparable or superior to that of ketoconazole. HQQ-3 retained potent activity against Candida albicans strains with low levels of susceptibility to fluconazole (fluconazole MIC80s range, 4 to >64 microg/ml). Against Cryptococcus neoformans and filamentous fungi, the activity of HQQ-3 was superior to that of fluconazole. HQQ-3 also exhibited potent in vivo activity against murine systemic infections caused by C. albicns and C. krusei. The 50% effective doses against these infections were 0.12 to 1.9 mg/kg of body weight. These result suggest that HQQ-3 may be useful in the treatment of candidiasis.
Zhao
Jing-Xia
JX
Department of Pharmacology, College of Pharmacy, Second Military Medical University, Shanghai, P R China.
Cao
Ying-Ying
YY
Quan
Hua
H
Liu
Chao-Mei
CM
He
Qiu-Qing
QQ
Wu
Qiu-Ye
QY
Gao
Ping-Hui
PH
Cao
Yong-Bing
YB
Liu
Wen-Xia
WX
Jiang
Yuan-Ying
YY
D000818:Animals; D000935:Antifungal Agents / Q000494:pharmacology* / Q000627:therapeutic use; D002177:Candidiasis / Q000188:drug therapy; D051379:Mice; D008826:Microbial Sensitivity Tests; D014230:Triazoles / Q000494:pharmacology* / Q000627:therapeutic use
D000935:Antifungal Agents; C515066:HQQ-3 compound; D014230:Triazoles