TUBERCULOSIS Synthetic Organic Compounds as Potential Antitubercular Drugs: A Review of the Progress Made in the Last Five Years
Pp. 231-266 (36)
Jean Leandro Santos, Guilherme F. dos Santos Fernandes, Priscila Longhin Bosquesi, Leonardo B. Marino, Clarice Q. F. Leite, Chung M. Chin and Fernando Rogério Pavan
Tuberculosis (TB) is an airborne infectious disease caused by
Mycobacterium tuberculosis (MTB) bacteria that is both preventable and curable.
Although the mortality rate has decreased worldwide, the emergence of multidrugresistant
MTB, extensively drug-resistant MTB, and MTB/human immunodeficiency
virus are stifling attempts to control TB and are associated with high rates of morbidity,
mortality, and impoverishment worldwide. Although the investment in research and
development has grown in recent years, the development of new candidate drugs has
not increased proportionally. Nevertheless, in the last few years we have seen some
evolution in the development of antitubercular drugs. After a gap of over 50 years
without any new drugs, several candidate drugs have been developed, offering new
hope for the treatment of drug-resistant strains of TB. Instead of focusing on recently
approved drugs or drugs close to approval, the objective of this review is to describe the
recent advances in the organic synthesis of drugs in early stages of development (hit-tolead)
that have shown good results in vitro in terms of the minimum inhibitory
concentration, median inhibitory concentration, and selectivity index.
Drug discovery, medicinal chemistry, tuberculosis.
Laboratory of Mycobacteriology “Prof. Dr. Hugo David”, Department of Biological Science, Faculty of Pharmaceutical Sicences, Paulista State University - UNESP, Rodovia Araraquara Jaú Km, 01, 14801-902 Araraquara, SP, Brazil.