Chemical Research Letters, May 2021. As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. , Name: 4-Methoxybenzene-1,3-diamine sulfate, 39156-41-7, Name is 4-Methoxybenzene-1,3-diamine sulfate, molecular formula is C7H12N2O5S, belongs to naphthyridine compound. In a document, author is Wang, Ming-Shu, introduce the new discover.
A potent and novel MET inhibitor, 5-((4((2-amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)amino)-3-(4-fluorophenyl)-1,6-naphthyridin-4(1H)-ones (8), was designed and synthesized via a scaffold-hopping strategy of a 2,7-naphthyridinone MET kinase inhibitor 7. Lead compound 8 had good potency (IC50 of 9.8 nM), but unfavorable pharmacokinetic profiles (F = 12%, CL = 5.0 L/h/kg). Systematic structural optimization of compound 8 resulted in 9g (MET, IC50 – of 9.8 nM) with a comparable MET potency to that of compound 2 and a favorable pharmacokinetic profile (F= 63%, CL = 0.12 L/h/kg). Further study of the derivatization of N(1) amine group of 9g led to the discovery of 23a with good MET potency (IC50 of 7.1 nM), promising VEGFR-2 selectivity (3226-fold), and a markedly drug-likeness improvement (F= 57.7%, CL = 0.02 L/h/kg). The excellent VEGFR-2 selectivity and favorable drug-likeness of 23g suggest that the 1,6-naphthyridine moiety could be used as a new scaffold for kinase inhibitor discovery. (C) 2019 Elsevier Masson SAS. All rights reserved.
The potential utility of systematic synthetic strategy will be applicable to efficient generations of chemical libraries of compounds to find ‘hit’ molecules. I hope my blog about 39156-41-7 is helpful to your research. Name: 4-Methoxybenzene-1,3-diamine sulfate.
Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem