328040-32-0Relevant academic research and scientific papers
Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A4 hydrolase
Kirkland, Thomas A.,Adler, Marc,Bauman, John G.,Chen, Ming,Haeggstroem, Jesper Z.,King, Beverly,Kochanny, Monica J.,Liang, Amy M.,Mendoza, Lisa,Phillips, Gary B.,Thunnissen, Marjolein,Trinh, Lan,Whitlow, Marc,Ye, Bin,Ye, Hong,Parkinson, John,Guilford, William J.
, p. 4963 - 4983 (2008/12/21)
Leukotriene B4 (LTB4) is a potent pro-inflammatory mediator that has been implicated in the pathogenesis of multiple diseases, including psoriasis, inflammatory bowel disease, multiple sclerosis and asthma. As a method to decrease the level of LTB4 and possibly identify novel treatments, inhibitors of the LTB4 biosynthetic enzyme, leukotriene A4 hydrolase (LTA4-h), have been explored. Here we describe the discovery of a potent inhibitor of LTA4-h, arylamide of glutamic acid 4f, starting from the corresponding glycinamide 2. Analogs of 4f are then described, focusing on compounds that are both active and stable in whole blood. This effort culminated in the identification of amino alcohol 12a and amino ester 6b which meet these criteria.
Novel and potent anti-malarial agents
Brinner, Kristin M,Mi Kim, Jin,Habashita, Hiromu,Gluzman, Ilya Y,Goldberg, Daniel E,Ellman, Jonathan A
, p. 3649 - 3661 (2007/10/03)
Readily accessible, novel, and potent anti-malarial compounds have been developed. Optimization of the initial lead structure resulted in derivatives with IC50 values from 7 to 35 nM against chloroquine-sensitive and 70-350 nM against chloroquine-resistant strains of Plasmodium falciparum.
