Name: m-Methoxyphenol. Xin, WX; Li, ZZ; Wang, Q; Du, J; Zhu, MY; Zhou, HC in [Xin, Weixiang; Li, Zezhong; Wang, Qing; Du, Jin; Zhu, Mingyan; Zhou, Huchen] Shanghai Jiao Tong Univ, Sch Pharm, State Key Lab Microbial Metab, Shanghai 200240, Peoples R China published Design and synthesis of alpha-phenoxy-N-sulfonylphenyl acetamides as Trypanosoma brucei Leucyl-tRNA synthetase inhibitors in 2020.0, Cited 18.0. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6.
Human African trypanosomiasis (HAT), caused by the parasitic protozoa Trypanosoma brucei, is one of the fatal diseases in tropical areas and current medicines are insufficient. Thus, development of new drugs for HAT is urgently needed. Leucyl-tRNA synthetase (LeuRS), a recently clinically validated antimicrobial target, is an attractive target for development of antitrypanosomal drugs. In this work, we report a series of alpha-phenoxy-N-sulfonylphenyl acetamides as T. brucei LeuRS inhibitors. The most potent compound 28g showed an IC50 of 0.70 mu M which was 250-fold more potent than the starting hit compound 1. The structure-activity relationship was also discussed. These acetamides provided a new scaffold and lead compounds for the further development of clinically useful antitrypanosomal agents. (C) 2019 Elsevier Masson SAS. All rights reserved.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles