192322-99-9

Upstream product

• 85-46-1 1-Naphthalenesulfonyl chloride 
• 1197-18-8 trans-4-aminomethyl-cyclohexyl-carboxylic acid 

Downstream Products

• 192323-20-9 toluene-4-sulfonic acid 4-[(naphthalene-1-sulfonylamino)-methyl]-cyclohexylmethyl ester 
• 192323-22-1 naphthalene-1-sulfonic acid [4-(2-amino-ethyl)-cyclohexylmethyl]-amide 
• 192323-00-5 4-[(naphthalene-1-sulfonylamino)-methyl]-cyclohexanecarboxylic acid amide 
• 192323-21-0 naphthalene-1-sulfonic acid (4-cyanomethyl-cyclohexylmethyl)-amide 
• 192323-01-6 naphthalene-1-sulfonic acid (4-aminomethyl-cyclohexylmethyl)-amide 
• 192323-04-9 naphthalene-1-sulfonic acid (4-amino-cyclohexylmethyl)-amide 
• 192323-19-6 naphthalene-1-sulfonic acid (4-hydroxymethyl-cyclohexylmethyl)-amide 

Relevant academic research and scientific papers

Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists

The design of a novel series of NPY-Y5 receptor antagonists is described. Key elements for the design were the identification of weak Y5 hits from a Y1 program, results from a combinatorial approach and database mining. This led to the discovery of the quinazoline 4 and the aryl-sulphonamide moiety as major components of the pharmacophore for Y5 affinity. The synthesis and SAR towards CGP71683A is described. (C) 2000 Elsevier Science Ltd. All rights reserved.

Synthesis and evaluation of new arylsulfonamidomethylcyclohexyl derivatives as human neuropeptide Y Y 5 receptor antagonists for the treatment of obesity

NPY is the most potent orexigenic peptide identified up to now. Stimulation of food intake is measured by the Y1 and Y5 receptor subtypes. In this study, the synthesis and evaluation of new arylsulfonamidomethylcyclohexyl derivatives are described as potential selective antagonists of the human NPY Y5 receptor. The SAR of these series was examined and the amide derivatives were the compounds that showed the best activities. trans-N-{4-[(Quinolin-3-yl)aminocarbonyl]cyclohexylmethyl}- 2,4-dichlorobenzenesulfonamide (42) bound to the human neuropeptide Y Y 5 receptor with a 2 nM IC50.

Synthesis and evaluation of new hydrazide derivatives as neuropeptide Y Y5 receptor antagonists for the treatment of obesity

NPY is the most potent orexigenic agent known to man, with NPY Y1 and NPY Y5 being the receptor subtypes that are most likely responsible for centrally-mediated NPY-induced feeding responses. Based on the aforementioned, novel hydrazide derivatives were prepared for the purpose of searching new NPY Y5 receptor antagonists. Many of the compounds exhibited nanomolar binding affinity for this receptor, affording trans-N-{4-[N′-(3,4-dichlorophenyl) hydrazinocarbonyl]cyclohexylmethyl}-4-fluorobenzenesulfonamide, which showed the best activity (IC50=0.43 nM). NPY is the most potent orexigenic agent known to man, with NPY Y1 and NPY Y5 being the receptor subtypes that are most likely responsible for centrally-mediated NPY-induced feeding responses. Based on the aforementioned, novel hydrazide derivatives were prepared for the purpose of searching new NPY Y5 receptor antagonists. Many of the compounds exhibited nanomolar binding affinity for this receptor, affording trans-N-{4-[N′-(3,4-dichlorophenyl)hydrazinocarbonyl]cyclohexylmethyl} -4-fluorobenzenesulfonamide, which showed the best activity (IC 50=0.43 nM).