《Discovery and structure activity relationships of 7-benzyl triazolopyridines as stable, selective, and reversible inhibitors of myeloperoxidase》 was written by Shaw, Scott A.; Vokits, Benjamin P.; Dilger, Andrew K.; Viet, Andrew; Clark, Charles G.; Abell, Lynn M.; Locke, Gregory A.; Duke, Gerald; Kopcho, Lisa M.; Dongre, Ashok; Gao, Ji; Krishnakumar, Arathi; Jusuf, Sutjano; Khan, Javed; Spronk, Steven A.; Basso, Michael D.; Zhao, Lei; Cantor, Glenn H.; Onorato, Joelle M.; Wexler, Ruth R.; Duclos, Franck; Kick, Ellen K.. Synthetic Route of C9H9BrO2This research focused ontriazolopyridine preparation myeloperoxidase inhibitor; structure arylmethyl aminophenylpropyl triazolopyridine inhibition myeloperoxidase selectivity; Atherosclerosis; Myeloperoxidase; Triazolopyridine. The article conveys some information:
Myeloperoxidase (MPO) is a heme peroxidase found in neutrophils, monocytes and macrophages that efficiently catalyzes the oxidation of endogenous chloride into hypochlorous acid for antimicrobial activity. Chronic MPO activation can lead to indiscriminate protein modification causing tissue damage, and has been associated with chronic inflammatory diseases, atherosclerosis, and acute cardiovascular events. A previously-known benzyloxy triazolopyrimidine was a reversible MPO inhibitor; however it suffered from poor stability in acid, and is an irreversible inhibitor of the DNA repair protein Me guanine Me transferase (MGMT). Structure-based drug design was employed to discover benzyl triazolopyridines such as I with improved MPO potency, as well as acid stability, no reactivity with MGMT, and selectivity against thyroid peroxidase (TPO). Structure-activity relationships, a crystal structure of the MPO-inhibitor complex, and acute in vivo pharmacodynamic data are described herein. In addition to this study using Methyl 3-(bromomethyl)benzoate, there are many other studies that have used Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Synthetic Route of C9H9BrO2) was used in this study.
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Synthetic Route of C9H9BrO2 Moreover, several studies demonstrate that the average proportion of bromine in drugs is significantly higher than that in natural products.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary