130944-47-7Relevant academic research and scientific papers
Divergent Supramolecular Gelation of Backbone Modified Short Hybrid δ-Peptides
Reja, Rahi M.,Patel, Rajat,Kumar, Vivek,Jha, Anjali,Gopi, Hosahudya N.
, p. 1254 - 1262 (2019)
The ordered supramolecular assemblies of short peptides have been recently gaining momentum due to their widespread applications in biology and materials sciences. In contrast to the α-peptides, limited success has been achieved from the backbone modified
INHIBITORS OF CYTOCHROME P450
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Paragraph 0872, (2015/11/10)
The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
Diastereoselective synthesis of a core fragment of ritonavir and lopinavir
Roy, Arnab,Reddy, Lekkala Amarnath,Dwivedi, Namrata,Naram, Jyothirmayi,Swapna, Rodda,Malakondaiah, Golla China,Ravikumar, Mylavarpu,Bhalerao, Dinesh,Pratap, Taduri Bhanu,Reddy, Padi Pratap,Bhattacharya, Apurba,Bandichhor, Rakeshwar
, p. 6968 - 6970 (2012/02/13)
A novel approach to the synthesis of Boc-core, a key starting material for ritonavir and lopinavir involving an unprecedented diastereoselective nitroaldol reaction on β-amino aldehyde is disclosed.
Kinetic deconjugation: A gateway to the synthesis of Xxx-Gly (E)-alkene dipeptide isosteres
Proteau-Gagné, Arnaud,Nadon, Jean-Franois,Bernard, Sylvain,Guérin, Brigitte,Gendron, Louis,Dory, Yves L.
supporting information; experimental part, p. 6603 - 6605 (2012/02/03)
A new method for the preparation of Xxx-Gly (E)-alkene dipeptide isosteres (EADIs), using LDA deprotonation followed by 1 N HCl quench, was explored. The method, named kinetic deconjugation, enabled the synthesis of Tyr-Gly, Gly-Gly, Ser-Gly, Pro-Gly, and
Synthesis and γ-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres
Nadin, Alan,Owens, Andrew P.,Castro, José L.,Harrison, Timothy,Shearman, Mark S.
, p. 37 - 41 (2007/10/03)
Two new APP substrate-based hydroxyethylene isosteres (AT and VI) were prepared and their dipeptide conjugates shown not to inhibit the γ-secretase-mediated formation of either Aβ1-40 or Aβ1-42. The FG isostere and a des-hydroxy hydroxyethylene isostere a
Synthesis of homochiral N-Boc-β-aminoaldehydes from N-Boc-β-aminonitriles
Toujas, Jean-Louis,Jost, Eric,Vaultier, Michel
, p. 713 - 718 (2007/10/03)
Enantiopure N-Boc-β-aminoaldehydes are efficiently prepared in good yields from N-Boc-β-aminonitriles by reduction of the nitrile function with diisobutylaluminium hydride (DIBAL-H) - Keywords: β-aminoaldehyde; β-aminonitrile; α-aminoacid; homochiral; enantiomeric excess; reduction; DIBAL-H
Aminodiol HIV Protease Inhibitors. 1. Design, Synthesis, and Preliminary SAR
Barrish, Joel C.,Gordon, Eric,Alam, Masud,Lin, Pin-Fang,Bisacchi, Gregory S.,et al.
, p. 1758 - 1768 (2007/10/02)
A series of HIV protease inhibitors containing a novel C2 symmetrical "aminodiol" core structure were prepared from amino acid starting materials.The ability of the aminodiols to inhibit HIV replication in cell culture is comparable to their ability to inhibit the isolated enzyme, a result compatible with good cell membrane penetration by this class of compounds.Optimization of the structure-activity in this series led to aminodiol 9a (Ki = 100 nM; ED50(HIV-1) = 80 nM) containing P1/P1' benzyl and P2/P2' Boc substituents.Compound 9a is a selective inhibito r of HIV protease versus other aspartyl proteases such as human renin, human cathepsin D, and porcine pepsin.In addition, 9a is equipotent against HIV-1 and HIV-2 in cell culture and demonstrates similar activity in infected T-lymphocytes and PBMCs.After iv and oral administration in rats, 9a displayed significant oral bioavailability (ca. 40percent) and a promising plasma elimination half-life (4 h).
A general route to "carba" peptide bond replacements: Unequivocal synthesis of Boc-L-Phe-ψ(CH2-CH2)-L-Ala-OH and Boc-L-Phe-ψ(CH2-CH2)-D-Ala-OH
Rodriguez, Marc,Aumelas, Andre,Martinez, Jean
, p. 5153 - 5156 (2007/10/02)
An unambiguous synthesis of Boc-L-Phe-ψ(CH2-CH2)-L-Ala-OH and BocL-Pheψ(CH2-CH2)-D-AlaOH from Boc-L-phenylalanine, through lactame intermediates (3R,6R)-3-m
Angiotensin-converting enzyme inhibitors: Synthesis and biological activity of acyl tripeptide analogues of enalapril
Greenlee,Allibone,Perlow,Patchett,Ulm,Vassil
, p. 434 - 442 (2007/10/02)
The synthesis and biological activity of a series of inhibitors of angiotensin-converting enzyme (EC 3.4.15.1) are described. Incorporation of the substituted N-carboxymethyl dipeptide design of enalapril (MK-421) into acyl tripeptides and larger peptides
