495401-20-2Relevant academic research and scientific papers
Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti-malaria Activity in Humanized Mice
Zhan, Wenhu,Zhang, Hao,Ginn, John,Leung, Annie,Liu, Yi J.,Michino, Mayako,Toita, Akinori,Okamoto, Rei,Wong, Tzu-Tshin,Imaeda, Toshihiro,Hara, Ryoma,Yukawa, Takafumi,Chelebieva, Sevil,Tumwebaze, Patrick K.,Lafuente-Monasterio, Maria Jose,Martinez-Martinez, Maria Santos,Vendome, Jeremie,Beuming, Thijs,Sato, Kenjiro,Aso, Kazuyoshi,Rosenthal, Philip J.,Cooper, Roland A.,Meinke, Peter T.,Nathan, Carl F.,Kirkman, Laura A.,Lin, Gang
supporting information, p. 9279 - 9283 (2021/03/18)
Plasmodium falciparum proteasome (Pf20S) inhibitors are active against Plasmodium at multiple stages—erythrocytic, gametocyte, liver, and gamete activation stages—indicating that selective Pf20S inhibitors possess the potential to be therapeutic, prophyla
MACROCYCLIC COMPOUNDS AS PROTEASOME INHIBITORS
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Paragraph 0437, (2019/05/02)
The compounds of the present invention are represented by the following compounds having Formula I and Formula (I'): where the substituents R1, R2, R2', R3, R4, R5, R', R", X, Y, and Z are as defined herein and where the substituents R1, R2, R3, R4, R5, R', R", X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.
New tripeptide-based macrocyclic calpain inhibitors formed by n-alkylation of histidine
Chen, Hongyuan,Jiao, Wanting,Jones, Matthew A.,Coxon, James M.,Morton, James D.,Bickerstaffe, Roy,Pehere, Ashok D.,Zvarec, Ondrej,Abell, Andrew D.
, p. 2473 - 2484 (2013/01/16)
Two new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the peptide backbone are linked by a bridge containing a 1,4-disubstituted 1H-imidazole, are reported. The structure with an aldehyde at the C-terminus and the i
INHIBITORS OF IAP
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Page/Page column 37, (2010/04/03)
The invention provides novel compounds that are inhibitors of IAPs having the general formula: wherein X1, X2, X3, Y, A, R1, R2, R3, R4, R4', R5, R5'/
Inhibitors of IAP
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Page/Page column 39, (2010/02/15)
The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.
A simple and convenient transformation of L-lysine into pyridinoline and deoxypyridinoline, two collagen cross-links of biochemical interest
Allevi, Pietro,Galligani, Matteo,Anastasia, Mario
, p. 1901 - 1910 (2007/10/03)
Starting from L-lysine as the only chiral building block, pyridinoline and deoxypyridinoline are efficiently synthesised, thus mimicking the postranscriptional formation of these collagen cross-links.
