2. Academic Validation
  3. Design and synthesis of selenazole-substituted ritonavir analogs

Design and synthesis of selenazole-substituted ritonavir analogs

  • Bioorg Med Chem Lett. 2018 Aug 1;28(14):2379-2381. doi: 10.1016/j.bmcl.2018.06.027.
Junfei Qiao 1,  Chuanfang Zhao 2,  Jun Liu 3,  Yuguo Du 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Environmental Chemistry and Eco-toxicology, Research Center for Eco-Environmental Sciences, Chinese Academy of Science, Beijing 100085, China; School of Chemistry and Chemical Engineering, University of Chinese Academy of Sciences, Beijing 100049, China.
  • 2 School of Chemistry and Chemical Engineering, University of Chinese Academy of Sciences, Beijing 100049, China.
  • 3 State Key Laboratory of Environmental Chemistry and Eco-toxicology, Research Center for Eco-Environmental Sciences, Chinese Academy of Science, Beijing 100085, China.
  • 4 State Key Laboratory of Environmental Chemistry and Eco-toxicology, Research Center for Eco-Environmental Sciences, Chinese Academy of Science, Beijing 100085, China; School of Chemistry and Chemical Engineering, University of Chinese Academy of Sciences, Beijing 100049, China. Electronic address: duyuguo@rcees.ac.cn.
PMID: 29934245 DOI: 10.1016/j.bmcl.2018.06.027
Abstract

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.

Keywords

Antiviral; One-pot reaction; Protease inhibitor; Ritonavir; Selenazole.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z