57699-57-7Relevant academic research and scientific papers
NON-PEPTIDIC BRS-3 AGONISTS
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Page 40, 41, (2008/06/13)
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).
Design of selective peptidomimetic agonists for the human orphan receptor BRS-3
Weber, Dirk,Berger, Claudia,Eickelmann, Peter,Antel, Jochen,Kessler, Horst
, p. 1918 - 1930 (2007/10/03)
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.
RETROVIRAL PROTEASE INHIBITING COMPOUNDS
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, (2008/06/13)
A retroviral protease inhibiting compound of the formula: STR1 is disclosed wherein R 1, R 2, R 5, R 6, Y m and Y' n are herein defined.
