Synthesis and antifungal activities in vitro of novel pyrazino [2,1-a] isoquinolin derivatives.
A series of novel pyrazino[2,1-a]isoquinolin compounds were designed and synthesized, and their antifungal activities in vitro were evaluated. The results showed that all of the compounds exhibited antifungal activities. Some of them exhibited stronger antifungal activities than that of lead compounds and among them compound 11b was the most potent one, which showed more potent than that of the active control fluconazole to the four of the five tested fungi. The studies presented here provide a new structural type for the development of novel antifungal agents.
Tang
Hui
H
Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
Zheng
Canhui
C
Lv
Jiaguo
J
Wu
Juan
J
Li
Yanan
Y
Yang
Hui
H
Fu
Bingyue
B
Li
Chuntong
C
Zhou
Youjun
Y
Zhu
Ju
J
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001232:Aspergillus fumigatus / Q000187:drug effects / Q000502:physiology; D002176:Candida albicans / Q000187:drug effects / Q000502:physiology; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology*
D000935:Antifungal Agents; D007546:Isoquinolines; D011719:Pyrazines