474295-91-5

Upstream product

• 107-30-2 chloromethyl methyl ether 
• 52085-14-0 4-benzoxy-salicylaldehyde 
• 95-01-2 2,4-Dihydroxybenzaldehyde 
• 100-39-0 benzyl bromide 

Downstream Products

• 1382722-63-5 4'-(benzyloxy)-2'-(methoxymethoxy)-2-nitro-1,2,3,6-tetrahydro-1,1'-biphenyl 
• 1382722-64-6 N-(4'-(benzyloxy)-2'-(methoxymethoxy)-1,2,3,6-tetrahydro-[1,1'-biphenyl]-2-yl)acetamide 
• 1382722-65-7 N-(4'-(benzyloxy)-2'-hydroxy-1,2,3,6-tetrahydro-[1,1'-biphenyl]-2-yl)acetamide 
• 1382722-67-9 2'-acetamido-4-(benzyloxy)-1',2',3',6'-tetrahydro-[1,1'-biphenyl]-2-yl trifluoromethanesulfonate 
• 1382749-01-0 N-(4'-(((3R,4S,5R)-3,4-dihydroxy-5-methoxy-6,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-3-(trifluoromethyl)-4'hydroxy-1,2,3,6-tetrahydro-[1,1':2',1-terphenyl]-2-yl)acetamide 
• 1382722-62-4 (Z)-4-(benzyloxy)-2-(methoxymethoxy)-1-(2-nitrovinyl)benzene 
• 1292810-96-8 2',4,4'-tribenzyloxy-2-(methoxymethoxy)stilbene 
• 1009814-10-1 2',4,4'-tribenzyloxy-2-(methoxymethoxy)stilbene 
• 474296-04-3 dimethyl-carbamic acid 1-[2-(4-nitro-phenoxy)-ethyl]-2,3-dihydro-1H-benzo[c]azepin-7-yl ester 

Relevant academic research and scientific papers

C-TERMINAL HSP90 INHIBITORS

Hsp90 C-terminal inhibitors and pharmaceutical compositions containing such compounds are provided. The compounds of the disclosure are useful for the treatment and/or prevention of neurodegenerative disorders such as diabetic peripheral neuropathy.

Synthesis and evaluation of novologues as C-terminal Hsp90 inhibitors with cytoprotective activity against sensory neuron glucotoxicity

Compound 2 (KU-32) is a first-generation novologue (a novobiocin-based, C-terminal, heat shock protein 90 (Hsp90) inhibitor) that decreases glucose-induced death of primary sensory neurons and reverses numerous clinical indices of diabetic peripheral neuropathy in mice. The current study sought to exploit the C-terminal binding site of Hsp90 to determine whether the optimization of hydrogen bonding and hydrophobic interactions of second-generation novologues could enhance neuroprotective activity. Using a series of substituted phenylboronic acids to replace the coumarin lactone of 2, we identified that electronegative atoms placed at the meta-position of the B-ring exhibit improved cytoprotective activity, which is believed to result from favorable interactions with Lys539 in the Hsp90 C-terminal binding pocket. Consistent with these results, a meta-3-fluorophenyl substituted novologue (13b) exhibited a 14-fold lower ED50 for protection against glucose-induced toxicity of primary sensory neurons compared to 2.

Molecular design of potent tyrosinase inhibitors having the bibenzyl skeleton

In order to develop water soluble tyrosinase inhibitors, bibenzyl xyloside 1 isolated from Chlorophytum arundinaceum (liliaceae), and its derivatives 2 and 3 were synthesized by using Wittig reaction and trichloroimidate glycosylation procedure as key steps. Xylosides 1-3 showed potent tyrosinase inhibitory activity with IC50s of 1.6, 0.43, and 0.73 μM, respectively, although each NMR data of synthetic bibenzyls was not identical to that of naturally occurring xyloside 1.

A conformational restriction approach to the development of dual inhibitors of acetylcholinesterase and serotonin transporter as potential agents for Alzheimer's disease

Alzheimer's disease (AD) has been treated with acetylcholinesterase (AChE) inhibitors such as donepezil. However, the clinical usefulness of AChE inhibitors is limited mainly due to their adverse peripheral effects. Depression seen in AD patients has been treated with serotonin transporter (SERT) inhibitors. We considered that combining SERT and AChE inhibition could improve the clinical usefulness of AChE inhibitors. In a previous paper, we found a potential dual inhibitor, 1, of AChE (IC50=101 nM) and SERT (IC50=42 nM), but its AChE inhibition activity was less than donepezil (IC50=10 nM). Here, we report the conformationally restricted (R)-18a considerably enhanced inhibitory activity against AChE (IC50=14 nM) and SERT (IC50=6 nM).

BENZYLAMINE ANALOGUE

A compound of the formula (I): [wherein R1 represents a C1-C6 alkyl group etc., R2 and R3 are the same or different and represent a hydrogen atom etc., Ra represents a C1-C6 alkyl group etc., Arom represents an aryl group etc., A represents a C1-C6 alkylene group, E represents a single bond, an oxygen atom, a sulfur atom etc., X1 and X2 are the same or different and represent an oxygen atom or a sulfur atom] or a pharmacologically acceptable salt or ester thereof.

FUNGAL CELL WALL SYNTHESIS GENE

A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed.Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.

Design and synthesis of dual inhibitors of acetylcholinesterase and serotonin transporter targeting potential agents for Alzheimer's disease.

Highly efficient acetylcholinesterase (AChE) and serotonin transporter (SERT) dual inhibitors, (S)-4 and (R)-13 were designed and synthesized on the basis of the hypothetical model of AChE active site. Both compounds showed potent inhibitory activities against AChE and SERT. [structure: see text]