Bobileva, Olga; Bobrovs, Raitis; Kanepe, Iveta; Patetko, Liene; Kalnins, Gints; Sisovs, Mihails; Bula, Anna L.; Grinberga, Solveiga; Boroduskis, Martins; Ramata-Stunda, Anna; Rostoks, Nils; Jirgensons, Aigars; Tars, Kaspars; Jaudzems, Kristaps published their research in ACS Medicinal Chemistry Letters in 2021. The article was titled 《Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate》.Related Products of 1129-28-8 The article contains the following contents:
Viral mRNA cap methyltransferases (MTases) are emerging targets for the development of broad-spectrum antiviral agents. In this work, we designed potential SARS-CoV-2 MTase Nsp14 and Nsp16 inhibitors by using bioisosteric substitution of the sulfonium and amino acid substructures of the cosubstrate S-adenosylmethionine (SAM), which serves as the Me donor in the enzymic reaction. The synthetically accessible target structures were prioritized using mol. docking. Testing of the inhibitory activity of the synthesized compounds showed nanomolar to submicromolar IC50 values for 5 compounds To evaluate selectivity, enzymic inhibition of the human glycine N-methyltransferase involved in cellular SAM/SAH ratio regulation was also determined, which indicated that the discovered compounds are nonselective inhibitors of the studied MTases with slight selectivity for Nsp16. No cytotoxic effects were observed; however, this is most likely a result of the poor cell permeability of all evaluated compounds The experimental part of the paper was very detailed, including the reaction process of Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Related Products of 1129-28-8)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals.Related Products of 1129-28-8 Organobromine compounds have fallen under increased scrutiny for their environmental impact.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary