Species-Selective Pyrimidineamine Inhibitors of Trypanosoma brucei S-Adenosylmethionine Decarboxylase was written by Volkov, Oleg A.;Brockway, Anthony J.;Wring, Stephen A.;Peel, Michael;Chen, Zhe;Phillips, Margaret A.;De Brabander, Jef K.. And the article was included in Journal of Medicinal Chemistry in 2018.Recommanded Product: 96558-78-0 This article mentions the following:
New therapeutic options are needed for treatment of human African trypanosomiasis (HAT) caused by protozoan parasite Trypanosoma brucei. S-Adenosylmethionine decarboxylase (AdoMetDC) is an essential enzyme in the polyamine pathway of T. brucei. Previous attempts to target this enzyme were thwarted by the lack of brain penetration of the most advanced series. Herein, the authors describe a T. brucei AdoMetDC inhibitor series based on a pyrimidineamine pharmacophore that the authors identified by target-based high-throughput screening. The pyrimidineamines showed selectivity for T. brucei AdoMetDC over the human enzyme, inhibited parasite growth in whole-cell assay, and had good predicted blood-brain barrier penetration. The medicinal chem. program elucidated structure-activity relationships within the series. Features of the series that were required for binding were revealed by determining the x-ray crystal structure of TbAdoMetDC bound to one analog. The pyrimidineamine series provides a novel starting point for an anti-HAT lead optimization. In the experiment, the researchers used many compounds, for example, 3-Bromo-5-chlorophenylamine (cas: 96558-78-0Recommanded Product: 96558-78-0).
3-Bromo-5-chlorophenylamine (cas: 96558-78-0) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Recommanded Product: 96558-78-0
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary