78269-85-9Relevant articles and documents
MITOCHONDRIA-TARGETING PEPTIDES
-
Page/Page column 57, (2019/07/19)
Disclosed are non-natural peptides useful for the treatment and prevention of ischemia-reperfusion injury (e.g., cardiac ischemia-reperfusion injury) or myocardial infarction.
Studies on the synthesis of peptides containing dehydrovaline and dehydroisoleucine based on copper-mediated enamide formation
Gille, Franziska,Kirschning, Andreas
, p. 564 - 570 (2016/04/08)
The preparation of peptide fragments containing dehydrovaline and dehydroisoleucine moieties present in the antibiotic myxovalargin is reported. Peptide formation is based on a copper-mediated C-N cross-coupling protocol between an acyl amide and a peptidic vinyl iodide. The presence of a neighboring arginine in the vinyl iodide posed a challenge with respect to the choice of the protecting group and the reaction conditions. It was found that ornithine - a suitable precursor - is better suited than arginine for achieving good yields for the C-N cross-coupling reaction. The optimized conditions were utilized for the synthesis of peptides 32, 33, 39 and 40 containing a neighboring ornithine as well as for the tripeptide 44 containing dehydroisoleucine with the correct stereochemistry.
NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
-
, (2015/03/06)
Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of the a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; conversion of the amide group in amino acid-3 on these scaffolds to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
ANTIVIRAL PROTEASE INHIBITORS
-
Page/Page column 491, (2008/06/13)
The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and /or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
HIV PROTEASE INHIBITING COMPOUNDS
-
Page/Page column 115, (2010/02/12)
A compound of the formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
HIV PROTEASE INHIBITING COMPOUNDS
-
Page/Page column 59, (2010/02/12)
A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
Stabilized thyroxine compounds
-
, (2008/06/13)
Throxinyldimethylphosphinate was invented as a prodrug to stabilize thyroxine, a drug widely used to treat hypothyroidism and depression. The presence of the dimethylphosphinate group at the phenolic hydroxyl of thyroxine is key to preventing thyroxine fr
Stabilized thyroxine compounds
-
, (2008/06/13)
Throxinyldimethylphosphinate was invented as a prodrug to stabilize thyroxine, a drug widely used to treat hypothyroidism. The presence of the dimethylphosphinate group at the phenolic hydroxyl of thyroxine is key to preventing thyroxine from decomposing
Synthesis and Evaluation of Novel Activated Mixed Carbonate Reagents for the Introduction of the 2-(Trimethylsilyl)ethoxycarbonyl(Teoc)-Protecting Group
Shute, Richard E.,Rich, Daniel H.
, p. 346 - 349 (2007/10/02)
The synthesis of 1-benzotriazole (Teoc-OBt) and 1-pyrrolidin-2,5-dione (Teoc-OSu) in high yields is reported.Both compounds are crystalline compounds that react with amino acids und