학술논문

Recycling and refurbishing old antitubercular drugs: the encouraging case of inhibitors of mycolic acid biosynthesis
Document Type
Report
Source
Expert Review of Anti-infective Therapy. April 2013, Vol. 11 Issue 4, p429, 12 p.
Subject
Argentina
United States
Language
English
ISSN
1478-7210
Abstract
One of the first approaches undertaken in the quest for antitubercular compounds was that of understanding the mechanism of action of old drugs and proposing chemical modifications or other strategies to improve their activity, generally lost to the mechanisms of resistance developed by Mycobacterium tuberculosis. A leading case was the work carried out on a set of compounds with proven activity on the essential pathway of the synthesis of mycolic acids. As a result, different solutions were presented, improving the activity of those inhibitors or producing novel compounds acting on the same molecular target(s), but avoiding the most common resistance strategies developed by the tubercle bacilli. This review focuses on the activity of those compounds, developed following the completion of the studies on several of the classic antitubercular drugs.
Author(s): Juan M Belardinelli [sup.1] [sup.2] , Héctor R Morbidoni [sup.[*]] [sup.3] Keywords : antitubercular prodrugs; avoiding drug resistance; drug development; fatty acid synthase type II inhibitors; Mycobacterium tuberculosis; mycolic [...]