Reference of 1,5-Dibromopentane. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 1,5-Dibromopentane, is researched, Molecular C5H10Br2, CAS is 111-24-0, about Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer’s disease. Author is Xie, Sai-Sai; Liu, Jing; Tang, Chunli; Pang, Chengyun; Li, Qing; Qin, Yuelian; Nong, Xiaojie; Zhang, Zhipeng; Guo, Jie; Cheng, Maojun; Tang, Weizhong; Liang, Ningsheng; Jiang, Neng.
A series of rasagiline-clorgyline hybrids was designed, synthesized and investigated in vitro for their inhibition of monoamine oxidase and amyloid-β aggregation. Most of compounds were found to be selective and highly potent hMAO-B inhibitors showing IC50 values in the nanomolar, and exhibited a moderate inhibition of amyloid-β aggregation. 7-((5-(methyl(prop-2-yn-1-yl)amino) pentyl)oxy)chroman-4-one (6j) was the most interesting compound identified in this research, endowed with higher hMAO-B potency (IC50 = 4 nM) and selectivity (SI > 25000) compared to the reference selective inhibitor rasagiline (IC50 = 141 nM, SI > 355), and exhibited good inhibitory activity against Aβ1-42 aggregation (40.78%, 25μM). Kinetic and mol. modeling studies revealed that 7-((5-(methyl(prop-2-yn-1-yl)amino) pentyl)oxy)chroman-4-one was a competitive reversible inhibitor for hMAO-B. Moreover, compound 7-((5-(methyl(prop-2-yn-1-yl)amino) pentyl)oxy)chroman-4-one displayed low toxicity and good neuroprotective effects in SH-SY5Y cell assay, and could penetrate the blood-brain barrier according to the parallel artificial membrane permeability assay. Pharmacokinetics assay revealed that 7-((5-(methyl(prop-2-yn-1-yl)amino) pentyl)oxy)chroman-4-one possessed good pharmacokinetic profiles after i.v. and oral administrations. Overall, these results highlighted that 7-((5-(methyl(prop-2-yn-1-yl)amino) pentyl)oxy)chroman-4-one was an effective and promising multitarget agent against Alzheimer’s disease.
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Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis