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 compound...

Full description

Saved in:
Bibliographic Details
Published in:Archiv der Pharmazie (Weinheim) 2010-06, Vol.343 (6), p.360-366
Main Authors: Tang, Hui, Zheng, Can-hui, Zhu, Ju, Fu, Bing-yue, Zhou, You-jun, Lv, Jia-guo
Format: Article
Language:English
Subjects:
1-a]isoquinolin
Antifungal
Antifungal Agents - chemical synthesis
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Candida - drug effects
Candida - enzymology
Cryptococcus neoformans - drug effects
Cryptococcus neoformans - enzymology
Cytochrome P-450 Enzyme Inhibitors
Drug Design
Fungi - drug effects
Fungi - enzymology
Isoquinolines - chemical synthesis
Isoquinolines - chemistry
Isoquinolines - pharmacology
Lanosterol 14α-demethylase
Microbial Sensitivity Tests
Models, Molecular
Molecular Structure
Pyrazines - chemical synthesis
Pyrazines - chemistry
Pyrazines - pharmacology
Pyrazino
Pyrazino[2,1‐a]isoquinolin
Sterol 14-Demethylase
Synthesis
Trichophyton - drug effects
Trichophyton - enzymology
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.200900279