The Pseudo-Symmetric
HIV-protease inhibitors
biological screening
heteroaryl carboxyamides
modeling
pseudo-symmetric core
synthesis
Journal
Biomolecules
ISSN: 2218-273X
Titre abrégé: Biomolecules
Pays: Switzerland
ID NLM: 101596414
Informations de publication
Date de publication:
26 10 2021
26 10 2021
Historique:
received:
20
09
2021
revised:
21
10
2021
accepted:
23
10
2021
entrez:
27
11
2021
pubmed:
28
11
2021
medline:
13
1
2022
Statut:
epublish
Résumé
Here, we report the synthesis, enzyme inhibition and structure-activity relationship studies of a new potent class of HIV-1 protease inhibitors, which contain a pseudo-symmetric hydroxyethylamine core and heteroarylcarboxyamide moieties. The simple synthetic pathway furnished nine compounds in a few steps with high yields. The compounds were designed taking into account our previous results on other series of inhibitors with different substituents at P' and P'' and different ways of linking them to the inhibitor core. Potent inhibitory activity was obtained with nanomolar IC
Identifiants
pubmed: 34827582
pii: biom11111584
doi: 10.3390/biom11111584
pmc: PMC8615997
pii:
doi:
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
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