4530-37-4Relevant academic research and scientific papers
Solar and Visible Light Assisted Peptide Coupling
Mishra, Abhaya K.,Parvari, Galit,Santra, Sourav K.,Bazylevich, Andrii,Dorfman, Ortal,Rahamim, Jonatan,Eichen, Yoav,Szpilman, Alex M.
supporting information, p. 12406 - 12412 (2021/04/05)
Amino acid and peptide couplings are widely used in fields related to pharma and materials. Still, current peptide synthesis continues to rely on the use of expensive, water sensitive, and waste-generating coupling reagents, which are often prepared in mu
Influence of the dipeptide linker configuration on the activity of PSMA ligands
Uspenskaya, Anastasiya A.,Machulkin, Alexey E.,Nimenko, Ekaterina A.,Shafikov, Radik R.,Petrov, Stanislav A.,Skvortsov, Dmitry A.,Beloglazkina, Elena K.,Majouga, Alexander G.
, p. 756 - 759 (2021/01/12)
Selective ligands of an urea-based prostate specific membrane antigen with a phenylalanine/tyrosine-based dipeptide linker and with a mingled chiral centers configuration and/or substituted aromatic fragments were prepared in seven steps by liquid- and in
Synthesis and Characterization of a Series of Orthogonally Protected l-Carnosine Derivatives
El-Dakdouki, Mohammad H.,Daouk, Nadine,Abdallah, Hiba
, p. 1 - 12 (2018/02/19)
l-Carnosine (β-alanyl-l-histidine) is an endogenous dipeptide that has been recognized for its broad spectrum of beneficial biological activities. However, the therapeutic utility of molecule has been hampered by its instability in human plasma (half-life
Diphenylsilane as a coupling reagent for amide bond formation
Sayes, Morgane,Charette, André B.
supporting information, p. 5060 - 5064 (2017/11/09)
A simple procedure for amide bond formation using diphenylsilane as a coupling reagent is described. This methodology enables the direct coupling of carboxylic acids with primary and secondary amines, releasing only hydrogen and a siloxane as by-products. Only one equivalent of each partner is needed, providing a more sustainable amidation method producing minimal wastes. This methodology was also extended to the synthesis of peptides and lactams by addition of Hünig's base (DIPEA) and 4-dimethylaminopyridine (DMAP).
High penetration prodrug compositions of peptides and peptide-related compounds
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Page/Page column 78, (2016/02/26)
The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of peptides and peptide-related compounds, which are capable of crossing biological barriers with higher penetration efficiency comparing t
PEG prodrug of gambogic acid: Amino acid and dipeptide spacer effects
Ding, Ya,Zhang, Peng,Tang, Xiao-Yan,Zhang, Can,Ding, Song,Ye, Hai,Ding, Qi-Long,Shen, Wen-Bin,Ping, Qi-Neng
experimental part, p. 1694 - 1702 (2012/08/08)
The clinical application of gambogic acid (GA), a natural component with promising antitumor activity, was limited due to its extremely poor aqueous solubility, rapid elimination in vivo, and wide biodistribution. To solve these problems, 30 poly(ethylene
Microwave-assisted chemical ligation of S-acyl peptides containing non-terminal cysteine residues
Hansen, Finn K.,Ha, Khanh,Todadze, Ekaterina,Lillicotch, Aaron,Frey, Alexander,Katritzky, Alan R.
supporting information; experimental part, p. 7162 - 7167 (2011/11/14)
An efficient approach for the synthesis of a series of S-acyl peptides containing internal cysteine residues has been developed and the chemical long-range ligation of these S-acyl peptides via 5-, 8-, 11- and 14-membered cyclic transition states has been
Guanidine hydrochloride as an organocatalyst for N-Boc protection of amino groups
Jahani, Fatemeh,Tajbakhsh, Mahmood,Golchoubian, Hamid,Khaksar, Samad
supporting information; experimental part, p. 1260 - 1264 (2011/04/15)
A simple and efficient method for the chemoselective N-Boc protection of the amine moiety in a variety of compounds is described using di-tert-butyl dicarbonate and guanidine hydrochloride as an organocatalyst in ethanol at 35-40°C. Selective mono-N-Boc protection of diamines and chemoselective protection of hydroxylamines without formation of any side products is achieved. Amino acids and peptides are N-Boc protected efficiently in excellent yields under convenient reaction conditions.
A convenient route to diversely substituted icosahedral closomer nanoscaffolds
Jalisatgi, Satish S.,Kulkarni, Vikas S.,Tang, Betty,Houston, Zachary H.,Lee, Mark W.,Hawthorne, M. Frederick
supporting information; scheme or table, p. 12382 - 12385 (2011/10/02)
The design and synthesis of icosahedral polyhedral borane closomer motifs based upon carbonate and carbamate anchoring groups for biomedical applications are described. Dodecacarbamate closomers containing easily accessible groups of interest at their linker termini were synthesized via activation of the B-OH vertices as aryl carbonates and their subsequent reaction with primary amines. Novel dodecacarbonate closomers were successfully synthesized for the first time by reacting [closo-B12(OH)12]2- with an excess of respective aryl chloroformates, utilizing relatively short reaction times, mild conditions and simple purification strategies, all of which had previously presented difficulties in closomer chemistry. This methodology for the 12-fold degenerate synthesis of carbonate and carbamate closomers will greatly facilitate further exploration of closomers as monodisperse nanomolecular delivery platforms.
Water-soluble tripeptide Aβ (9-11) forms amyloid-like fibrils and exhibits neurotoxicity
Naskar, Jishu,Drew, Michael G. B.,Deb, Ishani,Das, Sumantra,Banerjee, Arindam
supporting information; experimental part, p. 2625 - 2628 (2009/05/30)
(Chemical Equation Presented) A water-soluble, hydrophilic tripeptide GYE, having sequence identity with the N-terminal segment of amyloid peptides Aβ(9-11), upon self-association exhibits amyloid-like fibrils and significant neurotoxicity towards the Neu
