Name: 2-Amino-2-(4-isopropylphenyl)ethanolOn September 14, 2017 ,《Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi》 was published in Journal of Medicinal Chemistry. The article was written by Brand, Stephen; Ko, Eun Jung; Viayna, Elisabet; Thompson, Stephen; Spinks, Daniel; Thomas, Michael; Sandberg, Lars; Francisco, Amanda F.; Jayawardhana, Shiromani; Smith, Victoria C.; Jansen, Chimed; De Rycker, Manu; Thomas, John; MacLean, Lorna; Osuna-Cabello, Maria; Riley, Jennifer; Scullion, Paul; Stojanovski, Laste; Simeons, Frederick R. C.; Epemolu, Ola; Shishikura, Yoko; Crouch, Sabrinia D.; Bakshi, Tania S.; Nixon, Christopher J.; Reid, Iain H.; Hill, Alan P.; Underwood, Tim Z.; Hindley, Sean J.; Robinson, Sharon A.; Kelly, John M.; Fiandor, Jose M.; Wyatt, Paul G.; Marco, Maria; Miles, Timothy J.; Read, Kevin D.; Gilbert, Ian H.. The article contains the following contents:
Chagas’ disease, caused by the protozoan parasite Trypanosoma cruzi, is the most common cause of cardiac-related deaths in endemic regions of Latin America. There is an urgent need for new safer treatments because current standard therapeutic options, benznidazole and nifurtimox, have significant side effects and are only effective in the acute phase of the infection with limited efficacy in the chronic phase. Phenotypic high content screening against the intracellular parasite in infected VERO cells was used to identify a novel hit series of 5-amino-1,2,3-triazole-4-carboxamides (ATC). Optimization of the ATC series gave improvements in potency, aqueous solubility, and metabolic stability, which combined to give significant improvements in oral exposure. Mitigation of a potential Ames and hERG liability ultimately led to two promising compounds, one of which demonstrated significant suppression of parasite burden in a mouse model of Chagas’ disease. After reading the article, we found that the author used 2-Amino-2-(4-isopropylphenyl)ethanol(cas: 910443-18-4Name: 2-Amino-2-(4-isopropylphenyl)ethanol)
2-Amino-2-(4-isopropylphenyl)ethanol(cas: 910443-18-4) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Name: 2-Amino-2-(4-isopropylphenyl)ethanol
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