130858-97-8Relevant academic research and scientific papers
Rescuing biological activity from synthetic phakellistatin 19
Pelay-Gimeno, Marta,Meli, Alessandra,Tulla-Puche, Judit,Albericio, Fernando
, p. 9780 - 9788 (2013)
Phakellistatins is one of the families of Pro-rich cyclic peptides whose synthetic counterparts have revealed cytotoxicities that differ greatly from those displayed by their corresponding natural ones. This is also the case of the last member isolated fr
Full Sequence Amino Acid Scanning of θ-Defensin RTD-1 Yields a Potent Anthrax Lethal Factor Protease Inhibitor
Li, Yilong,Gould, Andrew,Aboye, Teshome,Bi, Tao,Breindel, Leonard,Shekhtman, Alexander,Camarero, Julio A.
, p. 1916 - 1927 (2017)
θ-Defensin RTD-1 is a noncompetitive inhibitor of anthrax lethal factor (LF) protease (IC50 = 390 ± 20 nM, Ki = 365 ± 20 nM) and a weak inhibitor of other mammalian metalloproteases such as TNFα converting enzyme (TACE) (Ki/sub
Direct Access to Acyl Fluorides from Carboxylic Acids Using a Phosphine/Fluoride Deoxyfluorination Reagent System
Munoz, Socrates B.,Dang, Huong,Ispizua-Rodriguez, Xanath,Mathew, Thomas,Prakash, G.K. Surya
supporting information, (2019/03/19)
A fast and simple method for deoxyfluorination of carboxylic acids is presented. The protocol employs commodity chemicals (PPh3, NBS, fluoride), affording products in excellent yields under mild conditions. Acyloxyphosphonium ion, the key reaction intermediate, was identified by NMR spectroscopic methods. Br?nsted acidic conditions are essential for efficient C-F bond formation. The protocol displays scalability, high functional group tolerance, chemoselectivity, and easy purification of products. Deoxyfluorination of active pharmaceutical ingredients was established.
Synthesis of Optically Active 2-Amino-1,3,4-oxadiazoles and their Hybrid Peptides
Madhu, Chilakapati,Prabhu, Girish,Pal, Rumpa,Guru Row,Sureshbabu, Vommina V.
, p. 1438 - 1446 (2015/10/06)
Synthesis of 2-amino-1,3,4-oxadiazole derivatives of Nα-Cbz(benzyloxycarbonyl)/Boc-protected amino/peptide acids under sonication is described. The conditions involved in the present protocol are simple, mild, and racemization free. The utility
Fmoc-based synthesis of peptide thioesters for native chemical ligation employing a tert -butyl thiol linker
Raz, Richard,Rademann, Joerg
supporting information; experimental part, p. 1606 - 1609 (2011/05/12)
tert-Butyl thioesters display an astonishing stability toward secondary amines in basic milieu, in contrast to other alkyl and aryl thioesters. Exploiting this enhanced stability, peptide thioesters were synthesized in a direct manner, applying a tert-butyl thiol linker for Fmoc-based solid-phase peptide synthesis.
5,5-Dimethylproline dipeptides: Anacid-stable class of pseudoproline
Van Lierop, Bianca J.,Jackson, W.Roy,Robinson, Andrea J.
experimental part, p. 5357 - 5366 (2010/08/13)
Commercially available Fmoc-protected L-amino acids were employed and coupled to L-allylglycine.Cross metathesis with 2-methyl-2-butene using second generation Grubbs' catalyst gave L-prenylglycine-containing dipeptides.Treatment with trifluoromethanesulf
A convenient synthesis of 1,3,4-thiadiazole and 1,3,4-oxadiazole based peptidomimetics employing diacylhydrazines derived from amino acids
Nagendra,Lamani, Ravi S.,Narendra,Sureshbabu, Vommina V.
body text, p. 6338 - 6341 (2011/01/04)
Synthesis of novel orthogonally protected 1,3,4-thiadiazole and 1,3,4-oxadiazole tethered dipeptide mimetics is described. Both the heterocycles are prepared via a set of diacylhydrazines derived from amino acids. 1,3,4-Thiadiazoles are synthesized by deh
Synthesis and use of amino acid fluorides as peptide coupling reagents
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, (2008/06/13)
The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: STR1 or the acid fluoride salts thereof wherein BLK is an N-amino protecting group AA is an amino acid residue and X is H or a protecting group useful, and the first amino and peptide have a free amino group and a blocked carboxy end.
