In 2018,Ramsbeck, Daniel; Hamann, Antje; Richter, Georg; Schlenzig, Dagmar; Geissler, Stefanie; Nykiel, Vera; Cynis, Holger; Schilling, Stephan; Buchholz, Mirko published 《Structure-Guided Design, Synthesis, and Characterization of Next-Generation Meprin β Inhibitors》.Journal of Medicinal Chemistry published the findings.Recommanded Product: Methyl 3-(bromomethyl)benzoate The information in the text is summarized as follows:
The metalloproteinase meprin β emerged as a current drug target for the treatment of a number of disorders, among those fibrosis, inflammatory bowel disease and Morbus Alzheimer. A major obstacle in the development of metalloprotease inhibitors is target selectivity to avoid side effects by blocking related enzymes with physiol. functions. Here, we describe the structure-guided design of a novel series of compounds, based on previously reported highly active meprin β inhibitors. The bioisosteric replacement of the sulfonamide scaffold gave rise to a next generation of meprin inhibitors. Selected compounds based on this novel amine scaffold exhibit high activity against meprin β and also remarkable selectivity over related metalloproteases, i.e., matrix metalloproteases and A disintegrin and metalloproteinases. In the experiment, the researchers used many compounds, for example, Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Recommanded Product: Methyl 3-(bromomethyl)benzoate)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals.Recommanded Product: Methyl 3-(bromomethyl)benzoate Organobromine compounds have fallen under increased scrutiny for their environmental impact.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary