Design, synthesis, and antiviral activity of phenylalanine derivatives as HIV-1 capsid inhibitors.
Anti-HIV Agents
/ chemical synthesis
Capsid Proteins
/ antagonists & inhibitors
Cells, Cultured
Dose-Response Relationship, Drug
Drug Design
HIV-1
/ drug effects
Humans
Microbial Sensitivity Tests
Molecular Dynamics Simulation
Molecular Structure
Phenylalanine
/ chemical synthesis
Structure-Activity Relationship
Virus Replication
/ drug effects
HIV-1 CA inhibitors
HIV-1 Capside Protein
PF-74 derivative
Scaffold Hopping
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
15 10 2021
15 10 2021
Historique:
received:
21
06
2021
revised:
07
09
2021
accepted:
09
09
2021
pubmed:
26
9
2021
medline:
13
1
2022
entrez:
25
9
2021
Statut:
ppublish
Résumé
The HIV-1 Capsid (CA) is considered as a promising target for the development of potent antiviral drugs, due to its multiple roles during the viral life cycle. Herein, we report the design, synthesis, and antiviral activity evaluation of series of novel phenylalanine derivatives as HIV-1 CA protein inhibitors. Among them, 4-methoxy-N-methylaniline substituted phenylalanine (II-13c) and indolin-5-amine substituted phenylalanine (V-25i) displayed exceptional anti-HIV-1 activity with the EC
Identifiants
pubmed: 34562701
pii: S0968-0896(21)00422-3
doi: 10.1016/j.bmc.2021.116414
pmc: PMC9127657
mid: NIHMS1799873
pii:
doi:
Substances chimiques
Anti-HIV Agents
0
Capsid Proteins
0
Phenylalanine
47E5O17Y3R
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
116414Subventions
Organisme : NIAID NIH HHS
ID : R01 AI150491
Pays : United States
Organisme : NIGMS NIH HHS
ID : R01 GM125396
Pays : United States
Organisme : NIMH NIH HHS
ID : T32 MH079785
Pays : United States
Informations de copyright
Copyright © 2021 Elsevier Ltd. All rights reserved.
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