| Development of 5-amino-1H-pyrazole-4-carboxamide derivatives as a possible therapeutic new class against human respiratory viruses and perspectives in the drug design for new emerging SARS-CoV-2 infection |
| Paper ID : 1062-ISCH |
| Authors |
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Ayman Abdelfattah Bastawy Farag *1, Galal Elgemeie2, Ahmed Samir3, Nasra Abdel fattah4, Samah loutfy4 1Pharmaceutical chemistry Department, Ahram Canadian University 2Chemistry Department, Faculty of Science, Helwan University, Helwan, Cairo, Egypt 3Nanotechnology research center, British University in Egypt, Cairo, Egypt 4Virology&Immunology unit, Cancer Biology Department, National Cancer Institute, Cairo University, Giza |
| Abstract |
| For the development of new derivatives against human respiratory viruses, a novel series of 5-amino-1H-pyrazole-4-carboxamide were synthesized. Furthermore, molecular docking studies of these compounds were carried to investigate their binding pattern with the prospective target, spike protein (PDB ID: 6mj0). Based on the In silico studies, the newly synthesized compounds were evaluated in vitro for their cytotoxicity and calculation of CC50 values to investigate their antiviral activities. The antiviral activities were evaluated against some respiratory viruses including human adenovirus and SARS-CoV2. Regarding, human adenoviruses, all tested compounds were evaluated for their antiviral activities using two mechanisms (adsorption and virucidal). Some of the tested compounds demonstrated strong anti-viral activities as evidenced by undetected viral copies in the infected cultures using quantitative real time PCR assay. In addition, some of the tested compounds showed antiviral activity against SARS-CoV2, evidence by high % of binding inhibition between spike protein and ACE2 protein using ELISA assay. |
| Keywords |
| 5-amino-1H-pyrazole-4-carboxamide, SARS-CoV-2 |
| Status: Abstract Accepted (Poster Presentation) |