3430-04-4

Upstream product

• 498-02-2 1-(3-methoxy-4-hydroxyphenyl)ethanone 
• 110-52-1 1,4-dibromo-butane 

Downstream Products

• 1446339-57-6 (S)-3-{1-[4-(4-acetyl-2-methoxyphenoxy)butyl]piperidin-2-yl}pyridine oxalate 
• 111627-19-1 1-[4-[4-[4-[Bis(4-fluorophenyl)hydroxymethyl]-1-piperidinyl]butoxy]-3-methoxyphenyl]ethanone 
• 111626-80-3 1-[4-[4-[4[Bis(4-fluorophenyl)methyl]-1-piperidinyl]butoxy]-3-methoxyphenyl]ethanone 
• 144253-71-4 [4-[4-[3-[1,2-Benzisothiazol-3-yl]-8-azabicyclo[3.2.1]octan-8-yl]butoxy]-3-methoxyphenyl] ethanone hydrochloride 
• 144062-19-1 [4-[4-[3-[6-Flouro-1H-indazol-3-yl]-8-azabicyclo[3.2.1]octane-8-yl]butoxy]-3-methoxyphenyl]ethanone 
• 144253-67-8 [4-[4-[3-[6-fluoro-1,2-benzisoxazol-3-yl]-8-azabicyclo[3.2.1]octan-8-yl]butoxy]-3-methoxyphenyl] ethanone fumarate 
• 144253-62-3 [4-[4-[3-[1,2-benzisoxazol-3-yl]-8-azabicyclo[3.2.1 ]octan-8-yl]butoxy]-3-methoxyphenyl] ethanone hydrochloride 

Relevant academic research and scientific papers

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

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 (40.78percent, 25 μM). Kinetic and molecular modeling studies revealed that 6j was a competitive reversible inhibitor for hMAO-B. Moreover, compound 6j 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 compound 6j possessed good pharmacokinetic profiles after intravenous and oral administrations. Overall, these results highlighted that compound 6j was an effective and promising multitarget agent against Alzheimer's disease.

Application of propynylamine derivative in pharmacy

The invention discloses application of a propynylamine derivative in pharmacy. Shown by tests of the applicant, the derivative can selectively inhibit MAO-B, is remarkable in activity and can be usedfor preparing MAO-B inhibitors and drugs for preventing

Propargylamine derivative and synthesis method thereof

The invention discloses a series of propargylamine derivatives and a synthesis method thereof. The synthesis method of the derivative mainly comprises the following steps: (1) putting any one of the structures shown in the following formulas (A)-(E) and e

Synthesis of N-aryloxyalkylanabasine derivatives

N-Aryloxyalkylanabasine derivatives were prepared via the reaction of anabasine hydrochloride with various aryloxyhaloalkanes in the presence of potash in DMF. The reaction occurred with retention of the chiral center C-(2) of the piperidine group. Side products of bis(aryloxy)ethanes were characterized.

Arylalkylheterocyclic amines,N-substituted by aryloxyalkyl group in a method for allergy treatment

A method of inhibiting Type 1 allergic responses in a living animal body with substituted heterocyclic amines is disclosed wherein the active agents are expressed generally by the formula which includes certain known and certain known compounds: STR1 wherein P is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is --CH--, CH2 -- or STR2 n is zero or one and when Q is --CH-- and n is one, a double bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the α carbon and a carbon of the central heterocyclic amine ring; Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition, R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values: 2H-1-benzopyran-2-one,4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4H-1-benzopyran-4-one, 1,4-benzodioxanloweralkyl-2-yl or 1,1'-biphenyl-4-yl and the pharmaceutically acceptable salts thereof.