期刊
FUTURE MEDICINAL CHEMISTRY
卷 8, 期 3, 页码 311-324出版社
FUTURE SCI LTD
DOI: 10.4155/fmc.15.185
关键词
anti-infective; carbonic anhydrase; metalloenzyme; polyamine; protozoan; sulfamate; sulfonamide; thiol; Trypanosoma cruzi
资金
- EU
An alpha-carbonic anhydrases (CAs, EC 4.2.1.1) was recently discovered, cloned and characterized in the genome of the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease, a neglected but widespread tropical disease. Inhibition of this alpha-CAs (TcCA) with anions, sulfonamides, sulfamates, thiols and hydroxamates has been investigated in detail, with several low nanomolar in vitro inhibitors. Although the sulfonamides were the best in vitro inhibitors, they showed no ex vivo anti-T. cruzi activity, due to poor penetration. However, some thiols and hydroxamates acting as low nanomolar TcCA inhibitors also showed significant antitrypanosomal ex vivo activity, making this enzyme an attractive yet underexplored drug target for the management of Chagas disease.
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