期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 33, 期 1, 页码 286-289出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2017.1414808
关键词
Benzoxaborole; Trypanosoma cruzi; Leishmania donovani chagasi; protozoan carbonic anhydrases; inhibition
资金
- LabEx CheMISyst [ANR-10-LABX-05-01]
- (Agence Nationale de la Recherche)
A series of 6-substituted ureido- and thioureido-benzoxaboroles were investigated as inhibitors of carbonic anhydrases from Trypanosoma cruzi (TcCA), and Leishmania donovani chagasi (LdcCA). Both enzymes were inhibited by benzoxaboroles in the micromolar range. Preferential inhibitory potency against the beta-CA LdcCA versus the alpha-CA TcCA was observed with submicromolar inhibitory activities. Some derivatives displayed excellent inhibitory and selectivity profile over the ubiquitous and physiological relevant human off-target hCA II. This study provides a convincing opportunity to study benzoxaborole scaffold for the design of antiprotozoan potential drugs targeting the pathogen's carbonic anhydrases.
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