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Discovery and optimization of novel and potent allosteric HIV-1 integrase inhibitors with a spiro[indene] moiety
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DOI:10.1016/j.bmc.2025.118526.png)
Abstract
En 中文
• Allosteric HIV-1 integrase inhibitors with a spiro[indene] moiety were designed by a structure-based drug design approach. • By SAR exploration that focused on the efficacies against not only wild type but also polymorphisms and resistance mutations, we identified novel allosteric HIV-1 integrase inhibitors effective against many genetic polymorphisms. • Compound 38 f exhibited desired efficacy against major polymorphisms and resistance mutations, and also displayed preferable PK profiles.
Journal
B
IF:
3
Papers:
1.7W
Citations:
2.7W
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