Revisiting the dipeptidyl carboxypeptidase inhibitor captopril as a source of pan anti-trypanosomatid agents.
Bioorg Med Chem Lett
; 110: 129883, 2024 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-39013490
ABSTRACT
The protozoan parasites Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp. are responsible for continued propagation of neglected tropical diseases such as African sleeping sickness, Chagas disease and leishmaniasis respectively. Following a report that captopril targets Leishmania donovani dipeptidyl carboxypeptidase, a series of simple proline amides and captopril analogues were synthesized and found to exhibit 1-2 µM in vitro inhibition and selectivity against Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp. The results were corroborated with computational docking studies. Arguably, the synthetic proline amides represent the structurally simplest examples of in vitro pan antiprotozoal compounds.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Trypanosoma brucei brucei
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Trypanosoma cruzi
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Captopril
Limite:
Humans
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article