68453-55-4

Upstream product

• 122357-96-4 4-(diethylaminocarbonyl)benzoic acid methyl ester 
• 109-89-7 diethylamine 
• 1571-08-0 methyl 4-formylbenzoate 
• 2417-72-3 Methyl 4-(bromomethyl)benzoate 
• 13686-66-3 N,N-diethylaminodimethylsilane 

Downstream Products

• 91271-57-7 (4-((diethylamino)methyl)phenyl)methanol 
• 82413-58-9 4-[(diethylamino)methyl]-benzaldehyde 
• 62642-61-9 4-Diethylaminomethyl-benzoic acid hydrazide 
• 62642-59-5 4-diethylaminomethyl-benzoic acid 
• 80335-46-2 4-(Diethylaminomethyl)benzoyl chloride 
• 1392835-70-9 4-[(diethylamino)methyl]-N-hydroxybenzamide 

Relevant academic research and scientific papers

Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome

Disease-modifying therapies are needed for Fragile X Syndrome (FXS), as at present there are no effective treatments or cures. Herein, we report on a tetrahydroquinoline-based selective histone deacetylase 6 (HDAC6) inhibitor SW-100, its pharmacological a

Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents

In present study, 4-anilinoquinazolines scaffold, arylurea and tertiary amine moiety were combined to design, synthesize gefitinib analogs and discover novel anticancer agents. A series of 4-anilinoquinazoline derivatives (1, 2, 3 and 4) bearing arylurea and tertiary amine moiety at its 6-position were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against A431 cell and A549 cell. The SAR of the title compounds was discussed. The compounds 2d, 2i and 2j with potent antiproliferative activities were evaluated their inhibitory activity against EGFR-TK. Compound 2j displayed potent inhibitory activity against EGFR-TK. In addition, compound 2j, at 50 mg/kg, can completely inhibit cancer growth in established nude mouse A549 xenograft model in vivo. These results suggest that the 4-anilinoquinazoline derivatives bearing diarylurea and tertiary amino moiety at its 6-position can serve as anticancer agents and EGFR inhibitors.

3,4-Dihydro-1,3,5-triazin-2(1H)-ones as the First Dual BACE-1/GSK-3β Fragment Hits against Alzheimer's Disease

One of the main obstacles toward the discovery of effective anti-Alzheimer drugs is the multifactorial nature of its etiopathology. Therefore, the use of multitarget-directed ligands has emerged as particularly suitable. Such ligands, able to modulate different neurodegenerative pathways, for example, amyloid and tau cascades, as well as cognitive and neurogenic functions, are fostered to come. In this respect, we report herein on the first class of BACE-1/GSK-3β dual inhibitors based on a 3,4-dihydro-1,3,5-triazin-2(1H)-one skeleton, whose hit compound 1 showed interesting properties in a preliminary investigation. Notably, compound 2, endowed with well-balanced potencies against the two isolated enzymes (IC50 of 16 and 7 μM against BACE-1 and GSK-3β, respectively), displayed effective neuroprotective and neurogenic activities and no neurotoxicity in cell-based assays. It also showed good brain permeability in a pharmacokinetic assessment in mice. Overall, triazinone derivatives, thanks to the simultaneous modulation of multiple points of the diseased network, might emerge as suitable candidates to be tested in in vivo Alzheimer's disease models.

HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME

Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.

Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives

A new series of indanone and aurone derivatives have been synthesized and tested for in vitro AChE inhibitory activity by modified Ellman method. Most of them exhibit AChE inhibitory activities superior to rivastigmine. Further, the most potent compound 1g was selected to evaluate the effect on the acquisition and memory impairment by mice step-down passive avoidance test.

QUINOLIN-4-YLHYDRAZINE DERIVATIVES AS ANTIMALARIAL AGENT

Novel quinolyl and acridinylhydrazone compounds of formula (I), which present remarkable biological activity especially against the choloroquine-resistant Plasmodium falciparum strains, useful for the treatment and prevention of malaria infection are described herein.

Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains

A series of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones were synthesized and tested for their antimalarial properties. These compounds showed remarkable anti-plasmodial activity in vitro especially against chloroquine-resistant strains. Their pot

Lewis acid-catalyzed reductive amination of carbonyl compounds with aminohydrosilanes

The TiCl4-catalyzed reaction of aromatic carbonyl compounds with (dialkylamino)dimethylsilanes gave tertiary amines in moderate to high yields. The reductive amination of aliphatic aldehydes was effectively catalyzed by ZnI2. Methyl

Reduction of antides to amines via catalytic hydrosilylation by a rhodium complex

Reduction of a wide range of tertiary amides with 2 molar equivalents of diphenylsilane was promoted by 0.1 mol% of RhH(CO)(PPh3)3 at room temperature, affording the corresponding tertiary amines in high yields. The synthetic utility is demonstrated by chemoselective reductions of amides having functional groups such as ester and epoxy groups which are not tolerated by the conventional reductions with LiAlH4 and BH3.