Design and Synthesis of Potent Quinazolines as Selective β-Glucocerebrosidase Modulators was written by Zheng, Jianbin;Chen, Long;Schwake, Michael;Silverman, Richard B.;Krainc, Dimitri. And the article was included in Journal of Medicinal Chemistry in 2016.Quality Control of 4-Amino-1-methylpiperidine This article mentions the following:
Gaucher’s disease is a common genetic disease caused by mutations in the β-glucocerebrosidase (GBA1) gene that have been also linked to increased risk of Parkinson’s disease and Lewy body dementia. Stabilization of misfolded mutant β-glucocerebrosidase (GCase) represents an important therapeutic strategy in synucleinopathies. Here we report a novel class of GCase quinazoline inhibitors, obtained in a high throughput screening, with moderate potency against wild-type GCase. Rational design and a SAR study of this class of compounds led to a new series of quinazoline derivatives with single-digit nanomolar potency. These compounds were shown to selectively stabilize GCase when compared to other lysosomal enzymes and to increase N370S mutant GCase protein concentration and activity in cell assays. To the best of our knowledge, these mols. are the most potent noniminosugar GCase modulators to date that may prove useful for future mechanistic studies and therapeutic approaches in Gaucher’s and Parkinson’s diseases. In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4Quality Control of 4-Amino-1-methylpiperidine).
4-Amino-1-methylpiperidine (cas: 41838-46-4) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Quality Control of 4-Amino-1-methylpiperidine
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem