Design and optimization of piperidine-substituted thiophene[3,2-

Anti-HIV-1 drug candidate HIV-1 NNIBP NNRTIs Structural alert

Journal

Acta pharmaceutica Sinica. B
ISSN: 2211-3835
Titre abrégé: Acta Pharm Sin B
Pays: Netherlands
ID NLM: 101600560

Informations de publication

Date de publication:
Jul 2024
Historique:
received: 18 11 2023
revised: 26 02 2024
accepted: 11 03 2024
medline: 19 7 2024
pubmed: 19 7 2024
entrez: 19 7 2024
Statut: ppublish

Résumé

HIV-1 reverse transcriptase (RT) has received great attention as an attractive therapeutic target for acquired immune deficiency syndrome (AIDS), but the inevitable drug resistance and side effects have always been major challenges faced by non-nucleoside reverse transcriptase inhibitors (NNRTIs). This work aimed to identify novel chemotypes of anti-HIV-1 agents with improved drug-resistance profiles, reduced toxicity, and excellent druggability. A series of diarylpyrimidine (DAPY) derivatives were prepared

Identifiants

DOI: 10.1016/j.apsb.2024.03.021 PMID: 39027243 PMC: PMC11252457
pubmed: 39027243
doi: 10.1016/j.apsb.2024.03.021
pii: S2211-3835(24)00102-3
pmc: PMC11252457
doi:

Types de publication

Journal Article

Langues

eng

Pagination

3110-3124

Informations de copyright

© 2024 The Authors.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

Auteurs

Yanying Sun (Y)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

Zhenzhen Zhou (Z)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

Zhongling Shi (Z)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

Fabao Zhao (F)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

Minghui Xie (M)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

Zongji Zhuo (Z)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

Erik De Clercq (E)

Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, K.U. Leuven, Leuven B-3000, Belgium.

Christophe Pannecouque (C)

Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, K.U. Leuven, Leuven B-3000, Belgium.

Dongwei Kang (D)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province, Jinan 250012, China.

Peng Zhan (P)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province, Jinan 250012, China.

Xinyong Liu (X)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province, Jinan 250012, China.

Classifications MeSH