Pesci, Elisabetta published the artcileNovel Hits in the Correction of ΔF508-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein: Synthesis, Pharmacological, and ADME Evaluation of Tetrahydropyrido[4,3-d]pyrimidines for the Potential Treatment of Cystic Fibrosis, Computed Properties of 39546-32-2, the publication is Journal of Medicinal Chemistry (2015), 58(24), 9697-9711, database is CAplus and MEDLINE.
Cystic fibrosis (CF) is a lethal genetic disease caused by mutations of the gene encoding the cystic fibrosis transmembrane conductance regulator (CFTR) with a prevalence of the ΔF508 mutation. Whereas the detailed mechanisms underlying disease have yet to be fully elucidated, recent breakthroughs in clin. trials have demonstrated that CFTR dysfunction can be corrected by drug-like mols. On the basis of this success, a screening campaign was carried out, seeking new drug-like compounds able to rescue ΔF508-CFTR that led to the discovery of a novel series of correctors based on a tetrahydropyrido[4,3-d]pyrimidine core. These mols. proved to be soluble, cell-permeable, and active in a disease relevant functional-assay. The series was then further optimized with emphasis on biol. data from multiple cell systems while keeping physicochem. properties under strict control. Three mols. were found to have promising profiles, and among them I confirmed the low metabolic data observed with CYP3A4 also in the intrinsic clearance assay. The pharmacol. and ADME profile of this corrector series hold promise for the development of more efficacious compounds to be explored for therapeutic use in CF.
Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Computed Properties of 39546-32-2.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem