3524-86-5

Upstream product

• 110-52-1 1,4-dibromo-butane 
• 99-93-4 4-Hydroxyacetophenone 
• 111-24-0 1,5-dibromo-pentane 

Downstream Products

• 5736-89-0 1-(4-butoxyphenyl)ethan-1-one 

Relevant academic research and scientific papers

Optimization and preclinical evaluation of novel histamine H3 receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives

As a continuation of our search for novel histamine H3 receptor ligands, a series of new acetyl and propionyl phenoxyalkylamine derivatives (2–25) was synthesized. Compounds with three to four carbon atoms alkyl chain spacer, composed of six various 4N-substituted piperazine moieties were evaluated for their binding properties at human histamine H3 receptors (hH3R). In vitro test results proved the 4-pyridylpiperazine moiety as crucial element for high hH3R affinity (hH3R Ki = 5.2–115 nM). Moreover introduction of carbonyl group containing residues in the lipophilic part of molecules instead of branched alkyl substituents resulted in increased affinity in correlation to previously described series, whereas propionyl derivatives showed slightly higher affinities than those of acetyl (16 and 22 vs. 4 and 10; hH3R Ki = 5.2 and 15.4 nM vs. 10.2 and 115 nM, respectively). These findings were confirmed by molecular modelling studies, demonstrating multiple ligand-receptor interactions. Furthermore, pharmacological in vivo test results of compound 4 clearly indicate that it may affect the amount of calories consumed, thus act as an anorectic compound. Likewise, its protective action against hyperglycemia and the development of overweight has been shown. In order to estimate drug-likeness of compound 4, in silico and experimental evaluation of metabolic stability in human liver microsomes was performed.

Investigation of apoptosis based on fluorescence lifetime imaging microscopy with a mitochondria-targeted viscosity probe

Cell apoptosis detection based on the functionality changes of cellular organelles, such as mitochondria, offers a quantitative method compared to morphology-based detection. However, the conventional detection methods for potential variation of the mitoc

Design, synthesis, and anti-proliferative evaluation of 1: H -1,2,3-triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates in estrogen responsive and triple negative breast cancer cells

A series of 1H-1,2,3 triazole grafted tetrahydro-β-carboline-chalcone/ferrocenylchalcone conjugates were synthesized and in vitro evaluated against estrogen responsive (MCF-7) and triple negative (MDA-MB-231) breast cancer cells. Comparative analysis reve

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

Nickel-Catalyzed Multicomponent Coupling Reaction of Alkyl Halides, Isocyanides and H2O: An Expedient Way to Access Alkyl Amides

We herein describe a Ni-catalyzed multicomponent coupling reaction of alkyl halides, isocyanides, and H2O to access alkyl amides. Bench-stable NiCl2(dppp) is competent to initiate this transformation under mild reaction conditions, thus allowing easy operation and adding practical value. Substrate scope studies revealed a broad functional group tolerance and generality of primary and secondary alkyl halides in this protocol. A plausible catalytic cycle via a SET process is proposed based on preliminary experiments and previous literature.

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.

Adenine derivatives invert high glucose-induced thioredoxin-interacting protein overexpression

Overexpression of thioredoxin-interacting protein (TXNIP) is associated with reduced insulin sensitivity and β-cell apoptosis. We have previously shown that W2476 inhibited high glucose-induced TXNIP expression at both mRNA and protein levels in INS-1E ce

4-Aminoquinoline-ferrocenyl-chalcone conjugates: Synthesis and anti-plasmodial evaluation

A series of aliphatic and aromatic substituted 1H-1,2,3-triazole-tethered 4-amino-quinoline-ferrocenylchalcone conjugates has been synthesized and evaluated for anti-plasmodial activity. The conjugates with flexible aliphatic (aminoethanol or aminopropano

Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation

A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50 values from 0.41 to 2.38?μ