الفهرس 
Synthesis of Some New Azines of Expected Biological Activity
AbstractOnly 14 pages are availabe for public view
 |  | from | 164 |  |  |
| | | from | 164 | | |
Abstract
Synthesis of a novel series of 6-amino-5-(benzo[d]thiazol-2-yl)-1-aryl-pyridones 8a-h and 8-(benzo[d]thiazol-2-yl)-2-aryl[1,2,4]triazolo[1,5-a]pyridones 14a-e through the reaction of 2-(benzo[d]thiazol-2-yl)-3-(dimethylamino)acrylonitrile 4 with each of N-arylcyanoacetamides 5a-h and 2-cyano-N’-(4-substituted benzylidene)acetohydrazides 9a-e, under conventional and grindstone methods. Additionally, a new chromen 17a-f and coumarin 18a-f analogs incorporated benzothiazole moiety were prepared by the reaction of 2-(benzo[d]thiazol-2-yl)acetonitrile 3 with 2-hydroxy-5-(aryldiazenyl)benzaldehyde derivatives 15a-f using green synthesis. The newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR and MS. All plausible mechanisms for their formation were discussed. Compounds 8a-h and 14a-e exhibited remarkable anti-corona virus activity and the antiviral activity was evaluated for them in vitro. The antiviral examination revealed that compound 8g which contains fluorophenyl group; is the most potent anti-SARS-CoV-2 among the prepared series 8a-h with IC50 = 10.520 oM and SI = 0.05228. Also, the mechanism of action of compound 8g with promising antiviral activity for repurposing against COVID-19 was investigated. Additionally, compound 8g showed good fit interaction with the active site of Mpro (PDB ID: 6Y2F) of SARS-CoV-2 using molecular docking 2015.10 program. Moreover, some selected products were tested and evaluated as antimicrobial agents.UV-visible absorption spectra and fluorescence study of some selected products was demonstrated