Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres

DOI: 10.1016/S0960-894X(97)10054-3

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2635 - 2638 (1997)

Update date:2022-08-03

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Authors:

Choy, Nakyen

Choi, Ho-Il

Jung, Won Hee

Kim, Chung Ryeol

Yoon, Heungsik

Kim, Sung Chun

Lee, Tae Gyu

Koh, Jong Sung

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Article abstract of DOI:10.1016/S0960-894X(97)10054-3

Novel irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres were designed, synthesized, and kinetically characterized. A representative compound 2 displayed rapid, time-dependent inactivation of HIV-1 protease and high potency in cell culture with IC₅₀ of 6.6 nM.

Full text of DOI:10.1016/S0960-894X(97)10054-3

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