100927-09-1Relevant articles and documents
Synthesis of 3,5-disubstituted 1,2,4-oxadiazoles as peptidomimetic building blocks
Jakopin, ?iga,Ro?kar, Robert,Dolenc, Marija Sollner
, p. 1465 - 1468 (2007)
Twelve new 1,2,4-oxadiazole based compounds have been synthesized. Their structures contain a protected amine and a carboxyl or an ester group, and thus serve as potential peptidomimetic building blocks. The synthetic route is simple and mild conditions are used so that the chirality of the starting amino acids is retained.
BENZAMIDES OF PYRAZOLYL-AMINO-PYRIMIDINYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF
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Paragraph 00442, (2020/07/07)
Provided is a novel class of orally and/or topically available, selective and potent JAK inhibitors as safe and effective therapeutics against various diseases and disorders. More particularly, provided are pharmaceutical composition of these compounds and methods of their preparation and use thereof.
Total syntheses of bacillamide C and neobacillamide A; Revision of their absolute configurations
Martinez, Veronica,Davyt, Danilo
, p. 1572 - 1575 (2014/01/06)
The enantiospecific syntheses of both enantiomers of bacillamide C and neobacillamide A are described, along with the measurement of their optical activities, leading to the revision of the proposed absolute configurations of these natural products.
Discovery, biological evaluation, and structure-activity relationship of amidine based sphingosine kinase inhibitors
Mathews, Thomas P.,Kennedy, Andrew J.,Kharel, Yugesh,Kennedy, Perry C.,Nicoara, Oana,Sunkara, Manjula,Morris, Andrew J.,Wamhoff, Brian R.,Lynch, Kevin R.,MacDonald, Timothy L.
experimental part, p. 2766 - 2778 (2010/09/04)
Sphingosine 1-phosphate (S1P), a potent phospholipid growth and trophic factor, is synthesized in vivo by two sphingosine kinases. Thus these kinases have been proposed as important drug targets for treatment of hyperproliferative diseases and inflammation. We report here a new class of amidine-based sphingosine analogues that are competitive inhibitors of sphingosine kinases exhibiting varying degrees of enzyme selectivity. These inhibitors display KI values in the submicromolar range for both sphingosine kinases and, in cultured vascular smooth muscle cells, decrease S1P levels and initiate growth arrest.