Discovery and Synthesis of Novel Bio-Isostere of Purine Analogues Inhibiting SARS-CoV-2 | ||||
| Egyptian Journal of Chemistry | ||||
| Volume 66, Issue 13, December 2023, Page 167-185 PDF (996.3 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ejchem.2023.196504.7681 | ||||
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| Authors | ||||
Reham A. Mohamed-Ezzat   1; Galal H. Elgemeie 2
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| 1Chemistry of Natural &Microbial Products Department, Pharmaceutical and Drug Industries Research Institute, National Research Center, Cairo, 12622, Egypt. | ||||
| 2Department 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. | ||||
| Keywords | ||||
| SARS-CoV2; COVID-19; anti-proliferative activity; purine analogs; N-cyanodithioiminocarbonate; triazolopyrimidines | ||||
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