2037-72-1

Upstream product

• 3173-53-3 Cyclohexyl isocyanate 
• 59477-34-8 4-(2-(benzamido)ethyl)benzenesulphonamide 
• 65-85-0 benzoic acid 
• 3741-66-0 Ethyl benzoyl carbonate 
• 2015-16-9 N-(4-[2-amino-ethyl]-benzenesulfonyl)-N'-cyclohexyl urea 
• 258262-54-3 tert-butyl (4-sulfamoyl phenethyl)carbamate 
• 35303-76-5 4-(2-aminoethyl)benzenesulfonamide 
• 98-88-4 benzoyl chloride 

Relevant academic research and scientific papers

Synthesis and evaluation of α-glucosidase inhibitory activity of sulfonylurea derivatives

Two series of sulfonylureas derivatives including 24 compounds (4, 7, 5a-5o, 8a-8h), among them 17 new derivatives, have been synthesized and evaluated for their α-glucosidase inhibitory activity. Compounds 5c, 5h and 8e showed significant in vitro α-glucosidase inhibition with IC50 values of 5.58, 79.85 and 213.36 μm, respectively, comparing with the standard compounds acarbose (IC50 = 268.29 μm) and glipizide (IC50 = 300.47 μm). The preliminary structure-activity relationships (SARs) of the synthesized compounds were also investigated.

Metal complex and pharmaceutical composition containing the same

A novel gold complex which has potent antitumor activity and is effective when administered in a smaller amount, and a medicinal composition containing the complex. The gold complex includes, as a ligand, (R,R,R)-cis,cis-spiro[4,4]nonane-1,6-diamine, which is represented by stereostructural formula (A).

Investigation of structure-activity relationships in a series of glibenclamide analogues

In this study, the synthesis of 15 new glibenclamide analogues is described. The conformational trends of these analogues were investigated using Monte Carlo conformational analysis. The conformational analysis results resolved the discrepancy between previous molecular modelling simulations of glibenclamide and allowed rationalizing the effect of aqueous environment on the overall conformation. The 3D-QSAR study was carried out with respect to the compounds' ability to antagonize the [3H]-glibenclamide binging in rat cerebral cortex. Superimposition of the antagonists was performed using the conformations derived from atom-by-atom fit to the glibenclamide crystal structure and this alignment was used to develop CoMFA models. CoMFA provided a good predictability: number of PLS components = 2, q2 = 0.876, R 2 = 0.921, SEE = 0.455 and F = 70. Best CoMFA models showed the steric and lipophilic properties as the major interacting forces whilst the electrostatic property contribution was a minor factor.