Identification of Boronate-Containing Diarylpyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.
DAPY
HIV-1
NNIBP
NNRTIs
boronate
drug design
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
03 Nov 2022
03 Nov 2022
Historique:
received:
06
10
2022
revised:
27
10
2022
accepted:
31
10
2022
entrez:
11
11
2022
pubmed:
12
11
2022
medline:
15
11
2022
Statut:
epublish
Résumé
In this study, privileged boronic acid ester was introduced into the right wing of etravirine (ETR) to obtain a series of novel boronate-containing derivatives. These newly synthesized derivatives were evaluated for their anti-HIV potency in MT-4 cells using the MTT method, and their inhibitory activity to HIV-1 reverse transcriptase (RT) was assayed by the ELISA method. Most of the synthesized compounds displayed promising antiviral activity against the wild-type and a wide range of HIV-1 mutant strains. In particular,
Identifiants
pubmed: 36364360
pii: molecules27217538
doi: 10.3390/molecules27217538
pmc: PMC9657321
pii:
doi:
Substances chimiques
Reverse Transcriptase Inhibitors
0
Anti-HIV Agents
0
HIV Reverse Transcriptase
EC 2.7.7.49
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : National Natural Science Foundation of China
ID : 82273773
Organisme : National Natural Science Foundation of China
ID : 82204215
Organisme : National Natural Science Foundation of China
ID : 81973181
Organisme : Shandong Provincial Natural Science Foundation
ID : ZR2021ZD17
Organisme : Shandong Provincial Natural Science Foundation
ID : ZR2021QH301
Organisme : Shandong Provincial Natural Science Foundation
ID : ZR2020JQ31
Organisme : Shandong Provincial Natural Science Foundation
ID : ZR2020YQ61
Organisme : Foreign Cultural and Educational Experts Project
ID : GXL20200015001
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