1217-60-3Relevant academic research and scientific papers
Structural requirements of acylated Gly- l -Ala- d -Glu analogs for activation of the innate immune receptor NOD2
Gobec, Martina,Mlinari?-Ra??an, Irena,Dolenc, Marija Sollner,Jakopin, Ziga
supporting information, p. 1 - 12 (2016/04/26)
The fragment of bacterial peptidoglycan muramyl dipeptide (MDP) has long been known for its adjuvant activity, however the underlying mechanism of this action has only recently been elucidated. It is ascribed to its agonist action on the nucleotide-bindin
Design and synthesis of calindol derivatives as potent and selective calcium sensing receptor agonists
Kiefer, Lionel,Beaumard, Floriane,Gorojankina, Tatiana,Faure, Hélène,Ruat, Martial,Dodd, Robert H.
, p. 554 - 569 (2016/02/09)
We report the first comprehensive structure-activity study of calindol (4, (R)-N-[(1H-indol-2-yl)methyl]-1-(1-naphthyl)ethanamine), a positive allosteric modulator, or calcimimetic, of the calcium sensing receptor (CaSR). While replacement of the naphthyl moiety of calindol by other aromatic groups (phenyl, biphenyl) was largely detrimental to calcimimetic activity, incorporation of substituents on the 4, 5 or 7 position of the indole portion of calindol was found to provide either equipotent derivatives compared to calindol (e.g., 4-phenyl, 4-hydroxy, 5-hydroxycalindol 44, 52, 53) or, in the case of 7-nitrocalindol (51), a 6-fold more active calcimimetic displaying an EC50 of 20 nM. Unlike calindol, the more active CaSR calcimimetics were shown not to act as antagonists of the closely related GPRC6A receptor, suggesting a more selective profile for these new analogues.
