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Letters in Organic Chemistry

Editor-in-Chief

ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

Research Article

Design, Synthesis and Biological Evaluation of Nucleozin Sulfonyl Piperazine Derivatives as Anti-influenza A Virus Inhibitors

Author(s): Shuchen Pei, Junlin Chen, Jinhua Yang, Lin Lai, Xiang Huang, Mingxin Xu and Jun Chen*

Volume 20, Issue 6, 2023

Published on: 20 October, 2022

Page: [501 - 506] Pages: 6

DOI: 10.2174/1570178619666220919102545

Price: $65

Abstract

Influenza A viruses have caused worldwide epidemics and pandemics by reassortment and generation of drug-resistant mutants, which leads to an urgent need to develop novel antivirals. In this study, a series of sulfonyl piperazine nucleozin derivatives were designed and synthesized, and their in vitro anti-influenza activity was evaluated. Many of these compounds exhibited moderate to good anti-influenza activity against influenza A. Among these, 6d, 6g, 6h, 6i, and 6j exhibited better activity than ribavirin. 2,3-dichlorobenzene substituted analogue 6i displayed the most remarkable in vitro activity against Influenza A. All the derivatives show no obvious cellular growth inhibition against MDCK cells. This study reported a new series of nucleoprotein inhibitors with a good selectivity window and potential for further development as novel anti-influenza agents.

Keywords: Anti-influenza A, Nucleoprotein, Sulfonyl Piperazine derivatives, Drug design, Synthesis, biological evaluation

Graphical Abstract

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