540483-63-4

Upstream product

• 163619-04-3 1-tert-butoxycarbonyl-N-[(9-fluorenyl)methoxycarbonyl]-D-tryptophan 
• 64-04-0 phenethylamine 
• 540483-62-3 N₁-phenethyl-(2R)-2-(9H-fluoren-9-ylmethoxy)-carboxamido-3-[1-(tert-butoxycarbonyl)-3-indolyl]-propanamide 

Downstream Products

• 540483-64-5 N₁-(2-phenylethyl)-(2R)-2-{[N'-((9H-fluoren-9-ylmethoxy)carbonyl)hydrazino]carboxamido}-3-[1-(tert-butoxycarbonyl)-3-indolyl]pronamide 
• 634163-29-4 C₂₅H₃₁N₅O₄ 
• 540483-72-5 N₁-(2-phenylethyl)-(2R)-2-{[(4-benzylpiperazino)methyl]carboxamido}-3-[1-(tert-butoxycarbonyl)-3-indolyl]propanamide 
• 540483-73-6 N₁-(2-phenylethyl)-(2R)-2-{[(4-benzylpiperidino)methyl]carboxamido}-3-[1-(tert-butoxycarbonyl)-3-indolyl]propanamide 

Relevant academic research and scientific papers

Design of selective peptidomimetic agonists for the human orphan receptor BRS-3

New tool substances may help to unravel the physiological role of the human orphan receptor BRS-3 and its possible use as a drug target for the treatment of obesity and cancer. In continuation of our work on BRS-3, the solid- and solution-phase synthesis of a library of low molecular weight peptidomimetic agonists based on the recently developed short peptide agonist 4 is described. Functional potencies of the compounds were determined measuring calcium mobilization in a fluorometric imaging plate reader (FLIPR) assay. Focusing on the N-terminus, the D-Phe-Gln moiety of 4 was modified in a combinatorial SAR-oriented medicinal chemistry approach. With the incorporation of N-arylated glycine and alanine building blocks azaglycine, piperazine, or piperidine and the synthesis of semicarbazides and semicarbazones, a number of highly potent and selective compounds with a reduced number of peptide bonds were obtained, which also should have enhanced metabolic stability.

NON-PEPTIDIC BRS-3 AGONISTS

The invention relates to novel compounds having a selective BRS-3 agonistic action and corresponding to general formula (I) wherein A1, A2, A3, R1, R2, R3, Ar1, Ar2, Ar3, m and n have the designations cited in the description. The invention also relates to pharmaceuticals containing said compounds and to methods for producing compounds of formula (I).