| Autor: |
Beatriz Vermelho, Alane, Rodrigues, Giseli Capaci, Nocentini, Alessio, Mansoldo, Felipe R. P., Supuran, Claudiu T. |
| Zdroj: |
Expert Opinion on Drug Discovery; October 2022, Vol. 17 Issue: 10 p1147-1158, 12p |
| Abstrakt: |
ABSTRACTIntroductionCarbonic anhydrase (CA) arose significant interest as a potential new target for Chagas disease since its discovery in Trypanosoma cruziin 2013. Benznidazole and Nifurtimox have been used for Chagas disease treatment for 60 years despite all efforts done for obtaining more efficient treatments, acting in the acute and chronic phases of illness, with fewer side effects and resistance induction.Areas coveredWe discuss the positive and negative aspects of T. cruziCA (TcCA) studies as a target for developing new drugs. The current research discoveries and the classes of TcCA inhibitors are reviewed. The sulfonamides and their derivatives are the main inhibitor classes, but hydroxamates and the thiols, were investigated too. These compounds inhibited the growth of the evolutive forms of the parasite. A comparative analysis was done with CAs from other Trypanosomatids and protozoans.Expert opinionThe search for new targets and drugs is a significant challenge worldwide, and TcCA is a potential candidate for developing new drugs. Several studied inhibitors were active against Trypanosoma cruzi, but their penetration and toxicity problems emerged. New approaches are in progress to obtain inhibitors with desired properties, allowing further steps such as tests using an adequate animal model and subsequent developments for the preclinical testing. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
|
