On October 8, 2015, Cleghorn, Laura A. T.; Albrecht, Sebastien; Stojanovski, Laste; Simeons, Frederick R. J.; Norval, Suzanne; Kime, Robert; Collie, Iain T.; De Rycker, Manu; Campbell, Lorna; Hallyburton, Irene; Frearson, Julie A.; Wyatt, Paul G.; Read, Kevin D.; Gilbert, Ian H. published an article.Safety of H-Idc-OH The title of the article was Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei. And the article contained the following:
There is an urgent need for new, brain penetrant small mols. that target the central nervous system second stage of human African trypanosomiasis (HAT). We report that a series of novel indoline-2-carboxamides have been identified as inhibitors of Trypanosoma brucei from screening of a focused protease library against Trypanosoma brucei brucei in culture. We describe the optimization and characterization of this series. Potent antiproliferative activity was observed The series demonstrated excellent pharmacokinetic properties, full cures in a stage 1 mouse model of HAT, and a partial cure in a stage 2 mouse model of HAT. Lack of tolerability prevented delivery of a fully curative regimen in the stage 2 mouse model and thus further progress of this series. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Safety of H-Idc-OH
The Article related to trypanosomicide indolinecarboxamide preparation structure activity brain penetrant trypanosomiasis, Pharmacology: Structure-Activity and other aspects.Safety of H-Idc-OH
Referemce:
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