《Synthesis and bioevaluation of 1-phenylimidazole-4-carboxylic acid derivatives as novel xanthine oxidoreductase inhibitors》 was written by Zhou, Haiyan; Li, Xiaolei; Li, Yuanyuan; Zhu, Xinying; Zhang, Lei; Li, Jing. Reference of Ethyl 2-amino-2-thioxoacetate And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
As part of a continuing study, author designed and synthesized four series of 1-phenylimidazole-4-carboxylic acid derivatives as xanthine oxidoreductase (XOR) inhibitors, evaluated their in vitro inhibitory potencies against XOR and hypouricemic effects in mice, and determined their structure-activity relationships (SARs). Most of the compounds exhibited in vitro XOR inhibition at the nanomolar level. In comparison to febuxostat (half-maximal inhibitory concentration [IC50] value of 7.0 nM), compounds I (R = (CH2)7) and II (R = 4-tBuC6H4, 4-MeOC6H4, 3-MeOC6H4) exhibited the most promising XOR inhibitory effects with IC50 values of 8.0 and 7.2 nM, resp. In the potassium oxonate/hypoxanthine-induced acute and long-term hyperuricemia mouse models, compounds I (R = (CH2)7) and II (R = 4-tBuC6H4, 4-MeOC6H4, 3-MeOC6H4) displayed significant hypouricemic potencies (P < 0.05), that were slightly weaker than and similar to febuxostat, resp. More interestingly, both compounds showed a capacity to improve kidney damage by decreasing creatinine and urea nitrogen levels compared to the long-term hyperuricemia mouse group (P < 0.05), while febuxostat showed no significant effect.Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Reference of Ethyl 2-amino-2-thioxoacetate) was used in this study.
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Reference of Ethyl 2-amino-2-thioxoacetate
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