Synthesis and evaluation of steroidal thiazoline conjugates as potential antiviral agents

Author:

Ke Shaoyong12,Li Ni3,Ke Ting4,Shi Liqiao1,Zhang Zhigang1,Fang Wei1,Zhang Ya-Ni1,Wang Kaimei1,Zhou Ronghua1,Wan Zhongyi1,Yang Ziwen1,Zhang Guangyang1,Wei Yanhong3

Affiliation:

1. National Biopesticide Engineering Research Centre, Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, Wuhan 430064, PR China

2. Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science & Technology, Shanghai 200237, PR China

3. Key Laboratory of Fermentation Engineering (Ministry of Education), Institute of Biomedical & Pharmaceutical Sciences, Hubei Provincial Cooperative Innovation Center of Industrial Fermentation, Hubei Key Laboratory of Industrial Microbiology, Sino–German Biomedical Center, National ‘111’ Center for Cellular Regulation & Molecular Pharmaceutics, Hubei University of Technology, Wuhan 430068, PR China

4. No. 1 Middle School of Lengji, Gucheng, Hubei 441703, PR China

Abstract

Aim: Many heterocyclic compounds derived from natural steroids exhibited broad activities, so this work focused on the investigations on a series of steroidal thiazoline conjugates as antiviral agents. Materials & methods: A series of steroid derivatives containing thiazoline heterocycles were designed and synthesized via a convenient condensation procedure. The compounds were screened for their potential antivirus activities against Enterovirus 71 (EV71) and Coxsackie Virus Type B (CVB3). Results and Conclusion: The in vitro bioassay indicated that compounds 5b, 5g and 5i exhibited excellent antiviral effects on EV71, and compounds 5b, 5e, 6c and 6g presented better antiviral activities against CVB3 compared with the controls ribavirin or pirodavir. These results indicate that these steroidal thiazoline conjugates might be feasible therapeutic candidates against EV71 infection, which might also be considered as promising compounds for optimization of potential antivirus agents.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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