344869-42-7Relevant academic research and scientific papers
Discovery and Optimization of a Compound Series Active against Trypanosoma cruzi, the Causative Agent of Chagas Disease
Harrison, Justin R.,Sarkar, Sandipan,Hampton, Shahienaz,Riley, Jennifer,Stojanovski, Laste,Sahlberg, Christer,Appelqvist, Pia,Erath, Jessey,Mathan, Vinodhini,Rodriguez, Ana,Kaiser, Marcel,Pacanowska, Dolores Gonzalez,Read, Kevin D.,Johansson, Nils Gunnar,Gilbert, Ian H.
, p. 3066 - 3089 (2021/06/14)
Chagas disease is caused by the protozoan parasite Trypanosoma cruzi. It is endemic in South and Central America and recently has been found in other parts of the world, due to migration of chronically infected patients. The current treatment for Chagas disease is not satisfactory, and there is a need for new treatments. In this work, we describe the optimization of a hit compound resulting from the phenotypic screen of a library of compounds against T. cruzi. The compound series was optimized to the level where it had satisfactory pharmacokinetics to allow an efficacy study in a mouse model of Chagas disease. We were able to demonstrate efficacy in this model, although further work is required to improve the potency and selectivity of this series.
Lithium borohydride: a reagent of choice for the selective reductive amination of cyclohexanones
Cabral, Shawn,Hulin, Bernard,Kawai, Makoto
, p. 7134 - 7136 (2008/03/11)
Traditional reductive amination of substituted cyclohexanones are either selective toward the formation of cis-products or show low selectivity. Herein we report a selective procedure for the reductive amination of substituted cyclohexanones with primary
A GENERAL, HIGHLY STEREOSELECTIVE SYNTHESIS OF AMINES
Wrobel, Jay E.,Ganem, Bruce
, p. 3447 - 3450 (2007/10/02)
The stereochemical course of cycloalkanone imine reductions by a variety of boron hydride reagents is described; very high stereoselectivity with substituted alkali metal borohydrides is reported.
