CIHIDECAR   12529
CENTRO DE INVESTIGACIONES EN HIDRATOS DE CARBONO
Unidad Ejecutora - UE
capítulos de libros
Título:
Targets and patented drugs for chemotherapy of Chagas disease
Autor/es:
DUSCHAK ,VILMA G.,; COUTO ALICIA S
Libro:
Frontiers in Anti-Infective Drug Discovery
Editorial:
Bentham Science Publishers
Referencias:
Año: 2010; p. 323 - 408
Resumen:
Chagas disease or American Trypanosomiasis, a parasitic infection
typically spread by triatomine bugs, affects millions of people throughout Latin
America. Current chemotherapy based on the nitroaromatic compounds, benznidazole
and nifurtimox provides unsatisfactory results and suffers from considerable
side effects and low efficacy. Therefore, there is an urgent need for new drugs to
treat this neglected disease.
Over the last two decades, new advances and understanding in the biology and the
biochemistry of Trypanosoma cruzi have allowed the identification of multiple
targets for Chagas´ disease chemotherapy. This chapter summarizes antichagasic
agents obtained based on i) target metabolic biochemical pathways or parasite
specific enzymes, ii) natural products and its derivatives, iii) design and synthesis
of lead compounds. Related patents filed and issued from 2000 to early 2009 are
also discussed. Most of them claimed inhibitors on specific parasite targets such as
cysteine proteinase, sterol biosynthesis, protein farnesyltransferase, etc. Particularly,
those related with cysteine proteinase inhibitors were the most represented.
Natural products also displayed many anti-T cruzi lead compounds. In addition, a
few patents claiming natural or synthetic compounds with antichagasic activity,
disclosed no specific target. However, only a small proportion of all these patents
displayed specific data of biological trypanocidal activity