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Discovery and optimization of novel and potent allosteric HIV-1 integrase inhibitors with a spiro[indene] moiety

delete2025-12-18
delete0
PRE
AI
K
Kaoru Adachi *
T
Tomoyuki Manabe
T
Takayuki Yamasaki
A
Akira Suma
Y
Yosuke Ogoshi
A
Akihiko Takahashi
T
Takuya Orita
A
Akihiro Nomura
T
Tsuyoshi Adachi
Y
Yoshitsugu Ohata
Y
Yoshiyuki Akiyama
S
Susumu Miyazaki
DOI:10.1016/j.bmc.2025.118526delete
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Abstract

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
Bioorganic and Medicinal Chemistry
IF:
3
Papers:
1.7W
Citations:
2.7W

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