Design and synthesis of novel pyrazino[2,1-a]isoquinolin derivatives with potent antifungal activity.
A series of novel pyrazino[2,1-a]isoquinolin compounds were designed, synthesized, and their antifungal activities in vitro were evaluated. The results showed that all of the title compounds exhibited antifungal activities. Most of them exhibited stronger antifungal activities than the lead compounds; compound 7c is more potent than fluconazole against two of the three tested fungal strains. The studies presented here provide a new structural type for the development of novel antifungal agents.
School of Pharmacy, Second Military Medical University, Shanghai, P R China.
Hui
H
Tang
Can-hui
CH
Zheng
Ju
J
Zhu
Bing-yue
BY
Fu
You-jun
YJ
Zhou
Jia-guo
JG
Lv
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002175:Candida / Q000187:drug effects / Q000201:enzymology; D003455:Cryptococcus neoformans / Q000187:drug effects / Q000201:enzymology; D065607:Cytochrome P-450 Enzyme Inhibitors; D015195:Drug Design; D005658:Fungi / Q000187:drug effects / Q000201:enzymology; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D058886:Sterol 14-Demethylase; D014249:Trichophyton / Q000187:drug effects / Q000201:enzymology
D000935:Antifungal Agents; D065607:Cytochrome P-450 Enzyme Inhibitors; D007546:Isoquinolines; D011719:Pyrazines; D058886:Sterol 14-Demethylase