55981-80-1Relevant academic research and scientific papers
A novel Zn-catalyzed hydroamination of propargylamides: A general synthesis of di- and tri-substituted imidazoles
Pews-Davtyan, Anahit,Beller, Matthias
supporting information; experimental part, p. 2152 - 2154 (2011/03/22)
Starting from commercially available amines and propargylamides a variety of substituted imidazoles were synthesized via a novel hydroamination- cyclization sequence. The target compounds are obtained in good to excellent yields in the presence of catalytic amounts of zinc triflate.
HIGH AFFINITY SMALL MOLECULE C5A RECEPTOR MODULATORS
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Page/Page column 131, (2010/02/06)
This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia) , 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at sub-nanomolar concentrations. Specifically exemplified representative compounds include, but are not limited to optionally substituted arylimidazoles, optionally substituted arylpyridyls, optionally substituted aryl-substituted cycloalkylimidazoles, optionally substituted arylpyrazoles, optionally substituted benzimidazoles, optionally substituted aryl-substituted tetrahydroisoquinolines, and optionally substituted biaryl carboxamides. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.
