120077-69-2Relevant articles and documents
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 00695, (2017/08/01)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 97, (2014/01/18)
This invention relates to novel spirocyclic piperidines according to Formula (I) which are inhibitors of fatty acid synthase (FAS), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Chemical subtleties in small-molecule modulation of peptide receptor function: The case of CXCR3 biaryl-type ligands
Wijtmans, Maikel,Scholten, Danny J.,Roumen, Luc,Canals, Meritxell,Custers, Hans,Glas, Marjolein,Vreeker, Marlies C.A.,De Kanter, Frans J.J.,De Graaf, Chris,Smit, Martine J.,De Esch, Iwan J.P.,Leurs, Rob
supporting information, p. 10572 - 10583 (2013/02/22)
The G protein-coupled chemokine receptor CXCR3 plays a role in numerous inflammatory events. The endogenous ligands for the chemokine receptors are peptides, but in this study we disclose small-molecule ligands that are able to activate CXCR3. A class of biaryl-type compounds that is assembled by convenient synthetic routes is described as a new class of CXCR3 agonists. Intriguingly, structure-activity relationship and structure-function relationship studies reveal that subtle chemical modifications on the outer aryl ring (e.g., either the size or position of a halogen atom) result in a full spectrum of agonist efficacies on CXCR3. Quantum mechanics calculations and nuclear Overhauser effect spectroscopy NMR studies suggest that the biaryl dihedral angle and the electronic nature of ortho-substituents play an important role in determining agonist efficacies. Compounds 38 (VUF11222) and 39 (VUF11418) are the first reported nonpeptidomimetic agonists on CXCR3, rendering them highly useful chemical tools for detailed assessment of CXCR3 activation as well as for studying downstream CXCR3 signaling.