In 2017,Zhao, Shizhen; Zhang, Xiangqian; Wei, Peng; Su, Xin; Zhao, Liyu; Wu, Mengya; Hao, Chenzhou; Liu, Chunchi; Zhao, Dongmei; Cheng, Maosheng published 《Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents》.European Journal of Medicinal Chemistry published the findings.Application of 16982-21-1 The information in the text is summarized as follows:
To further enhance the anti-Aspergillus efficacy of the authors’ previously discovered antifungal lead compounds (1), a series of aromatic heterocyclic derivatives were designed, synthesized and evaluated for in vitro antifungal activity. Many of the target compounds showed good inhibitory activity against Candida albicans and Cryptococcus neoformans. In particular, the isoxazole nuclei were more suited for improving the activity against Aspergillus spp. Among these compounds, 2-F substituted analogs isopropyl(S)-2-(5-(2-fluorophenyl)isoxazole-3-carboxamido)-3-(1H-imidazol-1-yl)propanoate and isobutyl(S)-2-(5-(2-fluorophenyl)isoxazole-3-carboxamido)-3-(1H-imidazol-1-yl)propanoate displayed the most remarkable in vitro activity against Candida spp., C. neoformans, A. fumigatus and fluconazole-resistant C.alb. strains, which is superior or comparable to the activity of the reference drugs fluconazole and voriconazole. Notably, the compounds isopropyl(S)-2-(5-(2-fluorophenyl)isoxazole-3-carboxamido)-3-(1H-imidazol-1-yl)propanoate and isobutyl(S)-2-(5-(2-fluorophenyl)isoxazole-3-carboxamido)-3-(1H-imidazol-1-yl)propanoate exhibited low inhibition profiles for various isoforms of human cytochrome P 450 and excellent blood plasma stability. The experimental process involved the reaction of Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Application of 16982-21-1)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Application of 16982-21-1
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics