10155-36-9

Upstream product

• 67-56-1 methanol 
• 1779-11-9 7-bromo-3-hydroxy-2-naphthoic acid 
• 74-88-4 methyl iodide 

Downstream Products

• 503827-85-8 UBP 617 
• 1333110-86-3 UBP 618 

Relevant academic research and scientific papers

Investigation of the structural requirements for N-methyl-D-aspartate receptor positive and negative allosteric modulators based on 2-naphthoic acid

The N-methyl-D-aspartate receptor (NMDAR), a ligand-gated ion channel activated by L-glutamate and glycine, plays a major role in the synaptic plasticity underlying learning and memory. NMDARs are involved in neurodegenerative disorders such as Alzheimer's and Parkinson's disease and NMDAR hypofunction is implicated in schizophrenia. Herein we describe structure-activity relationship (SAR) studies on 2-naphthoic acid derivatives to investigate structural requirements for positive and negative allosteric modulation of NMDARs. These studies identified compounds such as UBP684 (14b), which act as pan potentiators by enhancing NMDAR currents in diheteromeric NMDAR tetramers containing GluN1 and GluN2A-D subunits. 14b and derivatives thereof are useful tools to study synaptic function and have potential as leads for the development of drugs to treat schizophrenia and disorders that lead to a loss of cognitive function. In addition, SAR studies have identified a series of styryl substituted compounds with partial NAM activity and a preference for inhibition of GluN2D versus the other GluN2 subunits. In particular, the 3-and 2-nitrostyryl derivatives UBP783 (79i) and UBP792 (79h) had IC50s of 1.4 μM and 2.9 μM, respectively, for inhibition of GluN2D but showed only 70–80% maximal inhibition. GluN2D has been shown to play a role in excessive pain transmission due to nerve injury and potentially in neurodegenerative disorders. Partial GluN2D inhibitors may be leads for the development of drugs to treat these disorders without the adverse effects observed with full NMDAR antagonists.

Hydrazide derivatives and application thereof

The invention provides hydrazide derivatives and pharmaceutically acceptable salts thereof obtained through chemical synthesis. Pharmacological experiments prove that the compounds have the activity of resisting tumor cell proliferation, part of the compounds show the activity of inhibiting dimerization of protein DJ-1, and the compounds can be used for preparing drugs for treating, preventing andinhibiting DJ-1-associated tumor, type 2 diabetes as well as neurodegenerative diseases such as Parkinson s disease, Alzheimer's disease and the like. The general structural formula I of the compounds is shown in the description.

POSITIVE AND NEGATIVE MODULATORS OF NMDA RECEPTORS

Disclosed herein are compounds useful as modulators of an NMDA receptor. Further disclosed are methods of modulating an NMDA receptor using these compounds, and methods of treating various NMDA-receptor disorders, such as, for example, schizophrenia, post-traumatic stress disorder, Alzheimer's disease, and pain.

Enantioselective oxidative biaryl coupling reactions catalyzed by 1,5-diazadecalin metal complexes: Efficient formation of chiral functionalized BINOL derivatives

Chiral 1,5-diaza-cis-decalins have been examined as ligands in the enantioselective oxidative biaryl coupling of substituted 2-naphthol derivatives. Under the optimal conditions employing 2.5-10 mol % of a 1,5-diaza-cis-decalin copper(II) catalyst with oxygen as the oxidant, enantioselective couplings (44-96% ee) could be achieved for a range of 3-substituted 2-naphthols including the ester, ketone, phosphonyl, and sulfonyl derivatives. The relationship between the substitution of the naphthalene starting materials and reactivity/selectivity is determined by several factors which act in concert: (1) the effect of substituents on the oxidation potential of the substrate, (2) the ability of the substrate to participate in a chelated copper complex which depends on (a) the inherent coordinating ability of the 3-substituent and (b) substituent steric interactions that affect chelation between the 2-hydroxyl and 3-substituent, (3) the effect of substituents on dissociation of the product from the copper catalyst.

SULFURIC ACID ESTERS OF SUGAR ALCOHOLS

Compounds of the formula STR1 wherein n 1-n 9 are each independently 0 or 1;m 1-m 9 are each independently 0 or 1, but with the proviso that at least one of m 1, m 2 and m. sup.3, at least one of m 4, m 5 and m 6 and, when present, at least one of m 7, m 8 and m 9 is 1; and whereinX. sup.1-X 18 each independently is--O--,--CONR 1,--NR 1 CO--or--NR 1--;R 1 is hydrogen or lower alkyl;W is a benzene or s-triazine; Y. sup.1-Y 9 each independently is an aromatic ring systems;A 1-A 3 each independently is a residue of a sugar alcohol devoid of the 1-hydroxy group or a derivative thereof, a residue of a sugar acid devoid of the 1-carboxy group or a derivative thereof or tris-(hydroxymethyl)-methyl;D is the di-residue of a sugar alcohol devoid of 2 hydroxy groups or a derivative thereof or the di-residue of a sugar dicarboxylic acid devoid of 2 carboxy group or a derivative thereof;Q 1-Q. sup.3 and Z 1-Z3 each independently are the di-residue of a sugar alcohol devoid of 2 hydroxy groups or a derivative thereof or the di-residue of a sugar dicarboxylic acid devoid of 2 carboxy groups or a derivative thereof or didesoxyglycopyranoside or a derivative thereof, wherein at least one hydroxy group of residues A 1-A 3, D, Q 1-Q 3 and Z. sup.1-Z 3 is esterified with sulfuric acid, and pharmaceutically usable salts thereof are useful for the treatment of disorders which are characterized by excessive or destructive proliferation of smooth muscle cells.