Discovery of novel 1,2,4-triazole phenylalanine derivatives targeting an unexplored region within the interprotomer pocket of the HIV capsid protein.
HIV-1
capsid inhibitor
phenylalanine derivatives
scaffold hopping
target-based drug design
Journal
Journal of medical virology
ISSN: 1096-9071
Titre abrégé: J Med Virol
Pays: United States
ID NLM: 7705876
Informations de publication
Date de publication:
12 2022
12 2022
Historique:
revised:
20
07
2022
received:
09
06
2022
accepted:
08
08
2022
pubmed:
11
8
2022
medline:
18
10
2022
entrez:
10
8
2022
Statut:
ppublish
Résumé
Human immunodeficiency virus (HIV) capsid (CA) protein is a promising target for developing novel anti-HIV drugs. Starting from highly anticipated CA inhibitors PF-74, we used scaffold hopping strategy to design a series of novel 1,2,4-triazole phenylalanine derivatives by targeting an unexplored region composed of residues 106-109 in HIV-1 CA hexamer. Compound d19 displayed excellent antiretroviral potency against HIV-1 and HIV-2 strains with EC
Substances chimiques
Anti-HIV Agents
0
Capsid Proteins
0
Triazoles
0
1,2,4-triazole
288-88-0
Phenylalanine
47E5O17Y3R
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
5975-5986Subventions
Organisme : NIAID NIH HHS
ID : R01 AI150491
Pays : United States
Organisme : NIAID NIH HHS
ID : R01AI150491
Pays : United States
Informations de copyright
© 2022 Wiley Periodicals LLC.
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