Dihydropteridine-6 (5H)-ketone skeleton compound as well as preparation method and application thereof
By introducing a biaryl fragment and a pyrimidine ring into the diarylpyrimidine structure, the compound structure was optimized to enhance the nonpolar interaction with NNIBP, thus solving the problems of low bioavailability and drug resistance of ETR and RPV, and achieving highly efficient inhibition and low cytotoxicity against HIV-1 virus.
CN121991072APending Publication Date: 2026-05-08FUDAN UNIVERSITY
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Patent Information
- Application Number
- CN202610037956.1
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-01-13
- Publication Date
- 2026-05-08
AI Technical Summary
Technical Problem
Existing HIV reverse transcriptase inhibitors with diarylpyrimidine structures, ETR and RPV, suffer from low bioavailability, low patient response rates, and drug resistance, which limits their clinical application.
Method used
By introducing biaryl fragments and pyrimidine cyclic structures, compounds were optimized to enhance nonpolar interactions with amino acids within NNIBP. Compounds containing dihydropteridine-6(5H)-one skeletons were designed and synthesized to improve bioactivity against drug-resistant viral strains.
Benefits of technology
It significantly inhibits HIV-1 viral replication, exhibits low cytotoxicity and high selectivity, and enhances the inhibitory effect against drug-resistant viral strains.
✦ Generated by Eureka AI based on patent content.
Abstract
The invention belongs to the technical field of medicines, and particularly relates to a dihydropteridine-6 (5H)-ketone skeleton compound as well as a preparation method and application thereof. The dihydropteridine-6 (5H)-ketone skeleton compound disclosed by the invention is an HIV-1 (Human Immunodeficiency Virus-1) non-nucleoside reverse transcriptase inhibitor; the invention also comprises pharmaceutical salts, hydrates, solvates, polycrystals or co-crystals of the compounds, precursors and derivatives with the same biological functions of the compounds, a preparation method of the compounds and application of a composition containing one or more of the compounds in preparation of related drugs for treating AIDS and the like. The result of an in-vitro cellular level anti-HIV-1 activity experiment shows that the micromolecule has relatively strong anti-HIV-1 biological activity, can remarkably inhibit virus replication in MT-4 cells infected by HIV-1 viruses, and has relatively low cytotoxicity.
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