On the intrinsic reactivity of highly potent trypanocidal cruzain inhibitors.
Journal
RSC medicinal chemistry
ISSN: 2632-8682
Titre abrégé: RSC Med Chem
Pays: England
ID NLM: 101759460
Informations de publication
Date de publication:
18 Nov 2020
18 Nov 2020
Historique:
received:
28
03
2020
accepted:
03
08
2020
entrez:
7
6
2021
pubmed:
8
6
2021
medline:
8
6
2021
Statut:
epublish
Résumé
The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. Hence, peptidomimetic cruzipain inhibitors having a reactive group (known as warhead) are subject to continuous studies to discover novel antichagasic compounds. Here, we evaluated how different warheads for a set of structurally similar related compounds could inhibit the activity of cruzipain and, ultimately, their trypanocidal effect. We first investigated
Identifiants
pubmed: 34095840
doi: 10.1039/d0md00097c
pii: d0md00097c
pmc: PMC8126975
doi:
Types de publication
Journal Article
Langues
eng
Pagination
1275-1284Informations de copyright
This journal is © The Royal Society of Chemistry.
Déclaration de conflit d'intérêts
The authors declare no conflict of interest.
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