Discovery and Synthesis of Novel Bio-Isostere of Purine Analogues Inhibiting SARS-CoV-2

Document Type : Original Article

Authors

1 Chemistry of Natural &Microbial Products Department, Pharmaceutical and Drug Industries Research Institute, National Research Center, Cairo, 12622, Egypt.

2 Department of Chemistry, Faculty of Science, Helwan University, Cairo, 11795, Egypt.

Abstract

The pathogen SARS-CoV2 is extremely infectious. The novel SARS-CoV2 (2019-nCoV) virus that causes COVID-19 is resistant to the current antiviral medications, leading to an extremely high fatality rate. Millions of people have been affected by COVID-19 worldwide, and the number is dangerously rising due to the ongoing rise in cases. Toward developing SARS-COV-2 inhibitors, many pyrimidine and purine analogs have been depicted. Thus in order to developing new purine analogs the synthetic approach to prepare methylsulfanylpyrimidine nuclei is accomplished. Successful generation of a new series of triazolopyrimidines (TZP) as a new bio-isostere purine analog is furnished under mild conditions with high yields in a different manner from the traditional approaches and avoided the sophisticated methods. The crossponding triazolopyrazolopyrimidines which are characterized by the presence of tri-fused heterocyclic ring system were also produced. Selected compounds were tested for inhibition of SARS-CoV-2 viral replication. The antiproliferative efficacy of the newly synthesized compounds was also examined on a panel of NCI 60 human cancer cell lines. Our results demonstrated that the triazolopyrimidines 9b is a very promising novel purine analog that focus and highlights the potential of the TPZ scaffold as anti-CoV agent and is worthy of further evaluation as a potential therapeutic agent.

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Egyptian Journal of Chemistry
Volume 66, Issue 13 - Serial Number 13
Special Issue: Applied Chemistry for Greener Life and Sustainability
December 2023
Pages 167-185

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History

  • Receive Date: 04 March 2023
  • Revise Date: 20 April 2023
  • Accept Date: 01 May 2023

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