158478-81-0Relevant articles and documents
Preparation method of eptifibatide key raw material L-higher arginine
-
, (2021/02/20)
The invention discloses a preparation method of an eptifibatide key raw material L-higher arginine, and belongs to the field of synthesis of medical intermediates. The preparation method comprises thefollowing steps: reacting 1,3-bis(tert-butyloxycarbonyl)guanidine with p-toluenesulfonyl chloride to obtain 1,3-bis-Boc-2-(p-toluenesulfonyl)guanidine, then reacting the 1,3-bis-Boc-2-(p-toluenesulfonyl)guanidine with N-fluorenylmethoxycarbonyl-N'-tert-butyloxycarbonyl-L-lysine Fmoc-hArg(Boc2)-OH, removing Boc protection, and feeding Pbf-Cl to obtain N-(9-fluorenylmethoxycarbonyl)-2,2,4,6,7-pentamethyl-2H-benzofuran-5-sulfonyl-L-arginine. According to the invention, a p-toluenesulfonyl polypeptide guanidinylating agent is adopted in the route, so that ultralow-temperature reaction and the useof trifluoromethanesulfonyl chloride or trifluoromethanesulfonic anhydride with high corrosivity are avoided, and a simple and efficient way is provided for the synthesis of the intermediate.
RNA virus-derived peptides with modified side chains
-
Page/Page column 6; 7, (2013/09/12)
The present invention provides a RNA virus-derived peptides with modified side chains, wherein the side chains of the RNA virus-derived peptide are modified by altering the side-chain length or charges thereof such that the RNA virus-derived peptide has a high binding affinity for viral RNA and an high cellular uptake capability. The present invention also provides a composition for inhibiting RNA virus wherein the RNA virus-derived peptide can effectively inhibit viral self-replication and treat related diseases by its high affinity for viral RNA. A drug delivery carrier is also provided, wherein the RNA virus-derived peptides can carry desired drugs to the intracellular target due to its cellular uptake capability and thereby enhances the drug-delivery and treating efficiency.
Assessment of structurally diverse philanthotoxin analogues for inhibitory activity on ionotropic glutamate receptor subtypes: Discovery of nanomolar, nonselective, and use-dependent antagonists
Fr?lund, Sidsel,Bella, Angelo,Kristensen, Anders S.,Ziegler, Hanne L.,Witt, Matthias,Olsen, Christian A.,Str?mgaard, Kristian,Franzyk, Henrik,Jaroszewski, Jerzy W.
experimental part, p. 7441 - 7451 (2011/02/24)
An array of analogues of the wasp toxin philanthotoxin-433, in which the asymmetric polyamine moiety was exchanged for spermine and the headgroup replaced with a variety of structurally diverse moieties, was prepared using parallel solid-phase synthesis a