160357-86-8

Upstream product

• 452-07-3 2,4-difluorobenzyl chloride 
• 23915-07-3 1-(bromomethyl)-2,4-difluorobenzene 
• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 380423-91-6 1-(2,4-difluoro-benzyl)-piperidine-4-carboxylic acid amide 

Downstream Products

• 380425-83-2 2-chloro-6-[4-[1-(2,4-difluorobenzyl)]piperidinylamino]-9-cyclopentylpurine 

Relevant academic research and scientific papers

Heteroaryl compound and application thereof

The invention discloses a heteroaryl compound and application thereof, and provides a heteroaryl compound as shown in a formula I, a tautomer, a stereoisomer or a pharmaceutically acceptable salt thereof. The compound has good tumor inhibition activity, e

Rational Design and Multibiological Profiling of Novel Donepezil-Trolox Hybrids against Alzheimer's Disease, with Cholinergic, Antioxidant, Neuroprotective, and Cognition Enhancing Properties

A novel series of donepezil-trolox hybrids were designed, synthesized, and evaluated as multifunctional ligands against Alzheimer's disease (AD). Biological assays showed that these derivatives possessed moderate to good inhibitory activities against acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) as well as remarkable antioxidant effects. The optimal compound 6d exhibited balanced functions with good inhibition against hAChE (IC50 = 0.54 μM) and hMAO-B (IC50 = 4.3 μM), significant antioxidant activity (41.33 μM IC50 by DPPH method, 1.72 and 1.79 trolox equivalent by ABTS and ORAC methods), excellent copper chelation, and Aβ1-42 aggregation inhibition effect. Furthermore, cellular tests indicated that 6d has very low toxicity and is capable of combating oxidative toxin (H2O2, rotenone, and oligomycin-A) induced neurotoxicity. Most importantly, oral administration of 6d demonstrated notable improvements on cognition and spatial memory against scopolamine-induced acute memory deficit as well as d-galactose (d-gal) and AlCl3 induced chronic oxidative stress in a mouse model without acute toxicity and hepatotoxicity. In summary, both in vitro and in vivo results suggested that 6d is a valuable candidate for the development of a safe and effective anti-Alzheimer's drug.

The design and synthesis of purine inhibitors of CDK2. III

Cyclin-dependent kinases (CDKs) belong to a class of enzymes that control the ability of a cell to enter into and proceed through the cell division cycle. Using purine as a scaffold, we have synthesized a number of nanomolar inhibitors of CDK-2/cyclin E. In this report, the synthesis of a series of piperidine-substituted purine analogs will be presented, as well as some of their in vitro and in vivo biological effects.