《Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach》 was written by Steeneck, Christoph; Gege, Christian; Kinzel, Olaf; Albers, Michael; Kleymann, Gerald; Schlueter, Thomas; Schulz, Andreas; Xue, Xiaohua; Cummings, Maxwell D.; Fourie, Anne M.; Leonard, Kristi A.; Scott, Brian; Edwards, James P.; Hoffmann, Thomas; Goldberg, Steven D.. Name: Ethyl 2-amino-2-thioxoacetate And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020. The article conveys some information:
Starting from previously identified thiazole-2-carboxamides exemplified by compound I, two new series of RORγt inverse agonists with significantly improved aqueous solubility, ADME parameters and oral PK properties were discovered. These scaffolds were identified from a bioisosteric amide replacement approach. Amongst the variety of heterocycles explored, a 1,3,4-oxadiazole led to compounds with the best overall profile for SAR development and in vivo exploration. In an ex vivo mouse PD model, concentration dependent efficacy was demonstrated and compounds II and III were profiled in a 5-day rat tolerability study.Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Name: Ethyl 2-amino-2-thioxoacetate) was used in this study.
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Name: Ethyl 2-amino-2-thioxoacetate
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