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Expert Rev Anti Infect Ther ; 11(4): 429-40, 2013 Apr.
Article in English | MEDLINE | ID: mdl-23566152

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.


Subject(s)
Antitubercular Agents/chemical synthesis , Mycobacterium tuberculosis/drug effects , Mycolic Acids/antagonists & inhibitors , Antitubercular Agents/pharmacology , Drug Design , Drug Resistance, Multiple, Bacterial/drug effects , Ethionamide/analogs & derivatives , Ethionamide/chemical synthesis , Ethionamide/pharmacology , Humans , Isoniazid/analogs & derivatives , Isoniazid/chemical synthesis , Isoniazid/pharmacology , Mycobacterium tuberculosis/metabolism , Mycolic Acids/metabolism , Phenylthiourea/analogs & derivatives , Phenylthiourea/chemical synthesis , Phenylthiourea/pharmacology , Structure-Activity Relationship , Thioacetazone/analogs & derivatives , Thioacetazone/chemical synthesis , Thioacetazone/pharmacology , Tuberculosis, Pulmonary/drug therapy , Tuberculosis, Pulmonary/microbiology
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