Bioorganic and Medicinal Chemistry Letters p. 2379 - 2381 (2018)
Update date:2022-08-11
Topics:
Qiao, Junfei
Zhao, Chuanfang
Liu, Jun
Du, Yuguo
With the help of Surflex-Dock calculation, two ritonavir analogs in which one thioazole unit was replaced by selenazole have been designed and synthesized. The key selenazole structure was constructed from β-azido diselenide through a cascade diselenide cleavage/selenocarbonylation/Staudinger reduction/aza-Wittig reaction and a following MnO2 oxidation. The accordingly prepared compounds exhibited good anti-HIV-1 (IIIB) activities comparable to that of the original ritonavir, as well as the positive SI values.
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