1094375-93-5

Upstream product

• 173998-77-1 N-(tert-butyloxycarbonyl)-S-methylisothiourea 
• 1093949-60-0 4,4'-[1,4-phenylenebis(1H-1,2,3-triazole-4,1-diyl)]dibutanoic acid 

Downstream Products

• 1094375-88-8 di-tert-butyl (1,4-phenylenebis{1H-1,2,3-triazole-4,1-diyl(1-oxobutane-4,1-diyl)imino[(E)-({(4R)-5-[(4-tert-butoxybenzyl)amino]-4-[(diphenylacetyl)amino]-5-oxopentyl}amino)methylylidene]})biscarbamate 

Relevant academic research and scientific papers

Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists

According to a 'bivalent ligand approach' to increase the affinity of the potent argininamide-type NPY Y1 receptor antagonist BIBP-3226, dimeric ligands were synthesized in which two molecules of the parent compound were linked by different spacers via NG-acylation at the guanidino groups. A synthetic route for the preparation of the title compounds was developed, which includes a copper(I)-catalyzed azide alkyne cycloaddition as the key step. Three bivalent analogues of BIBP-3226 were prepared showing nanomolar antagonistic activity and binding affinity to the NPY Y1 receptor (calcium assay on HEL cells, radioligand binding assay on SK-N-MC cells), but these ligands were not superior to the parent compound and there was no correlation with the length or the chemical nature of the spacer. A trivalent BIBP-3226 derivate showed, surprisingly, no affinity to the NPY Y1 receptor at all.