《Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture》 was written by Kuehl, Nikos; Leuthold, Mila M.; Behnam, Mira A. M.; Klein, Christian D.. SDS of cas: 39546-32-2 And the article was included in Journal of Medicinal Chemistry on April 22 ,2021. The article conveys some information:
The viral serine protease NS2B-NS3 is one of the promising targets for drug discovery against dengue virus and other flaviviruses. The mol. recognition preferences of the protease favor basic, pos. charged moieties as substrates and inhibitors, which leads to pharmacokinetic liabilities and off-target interactions with host proteases such as thrombin. We here present the results of efforts that were aimed specifically at the discovery and development of noncharged, small-mol. inhibitors of the flaviviral proteases. A key factor in the discovery of these compounds was a cellular reporter gene assay for the dengue protease, the DENV2proHeLa system. Extensive structure-activity relationship explorations resulted in novel benzamide derivatives with submicromolar activities in viral replication assays (EC50 0.24μM), selectivity against off-target proteases, and negligible cytotoxicity. This structural class has increased drug-likeness compared to most of the previously published active-site-directed flaviviral protease inhibitors and includes promising candidates for further preclin. development. In the experiment, the researchers used many compounds, for example, Piperidine-4-carboxamide(cas: 39546-32-2SDS of cas: 39546-32-2)
Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.SDS of cas: 39546-32-2
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem