Souers, Andrew J. published the artcileSynthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3, Recommanded Product: 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, the main research area is G protein coupled receptor MCH antagonist alkoxy quinolinamine preparation; antiobesity agent melanin concentrating hormone receptor alkoxy quinolinamine preparation; obesity MCH antagonist melanin concentrating hormone receptor alkoxyquinolinamine preparation.
Prior SAR studies on 2-amino-8-alkoxyquinoline MCHr1 antagonists demonstrated that compounds with acyclic amide-containing sidechains displayed exceptional binding and functional potency, but negligible CNS penetration. Related analogs with acyclic benzylamine-containing sidechains showed greatly improved CNS exposure, but suffered in functional potency. In this report, it was demonstrated that cyclization of these benzylic amine sidechains affords compounds that combine the best elements of potency and CNS penetration among this class of antagonists. This is exemplified by 8-[[(3S)-1-(2,2-difluoro-1,3-benzodioxol-5-yl)-3-pyrrolidinyl]oxy]-2-quinolinamine (I), which has sub-nanomolar MCHr1 binding affinity, good functional potency, and excellent CNS exposure over 24 h.
Bioorganic & Medicinal Chemistry Letters published new progress about Antiobesity agents (antagonists). 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, Recommanded Product: 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem