In 2018,Gealageas, Ronan; Devineau, Alice; So, Pauline P. L.; Kim, Catrina M. J.; Surendradoss, Jayakumar; Buchwalder, Christian; Heller, Markus; Goebeler, Verena; Dullaghan, Edith M.; Grierson, David S.; Putnins, Edward E. published 《Development of Novel Monoamine Oxidase-B (MAO-B) Inhibitors with Reduced Blood-Brain Barrier Permeability for the Potential Management of Noncentral Nervous System (CNS) Diseases》.Journal of Medicinal Chemistry published the findings.Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide The information in the text is summarized as follows:
Studies indicate that MAO-B is induced in peripheral inflammatory diseases. To target peripheral tissues using MAO-B inhibitors that do not permeate the blood-brain barrier (BBB) the MAO-B-selective inhibitor deprenyl was remodeled by replacing the terminal acetylene with a CO2H function, and incorporating a para-OCH2Ar motif (compounds 10a-s). Further, in compound 32 ((S)-N-[1-cyano-3-[4-[(3,4-dichlorobenzyl)oxy]phenyl]propan-2-yl]-N-methylglycine hydrochloride) the C-2 side chain corresponded to CH2CN. In vitro, 10c (N-[(R)-[1-[4-(3-chlorobenzyloxy)phenyl]propan-2-yl](methyl)]glycine hydrochloride), 10j, 10k, and 32 were identified as potent reversible MAO-B inhibitors, and all four compounds were more stable than deprenyl in plasma, liver microsomal, and hepatocyte stability assays. In vivo, they demonstrated greater plasma bioavailability. Assessment of in vitro BBB permeability showed that compound 10k is a P-glycoprotein (P-gp) substrate and 10j displayed mild interaction. Importantly, compounds 10c, 10j, 10k, and 32 displayed significantly reduced BBB permeability after i.v., s.c., and oral administration. These polar MAO-B inhibitors are pertinent leads for evaluation of efficacy in noncentral nervous system (CNS) inflammatory disease models. The results came from multiple reactions, including the reaction of 2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide)
2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide