58578-45-3Relevant articles and documents
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
, 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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, (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.
Concise Synthesis of Enantiomerically Pure (1′S,2′R)-and (1′R,2′S)-2S-Amino-3-(2′-aminomethyl-cyclopropyl)propionic Acid: Two E-Diastereoisomers of 4,5-Methano-l-lysine
Altamore, Timothy M.,Nguyen, Oanh T. K.,Churches, Quentin I.,Cavanagh, Kate,Nguyen, Xuan T. T.,Duggan, Sandhya A. M.,Krippner, Guy Y.,Duggan, Peter J.
, p. 1105 - 1111 (2013/09/24)
A concise synthesis of both E-isomers of 2S-amino-3-(2′-aminomethyl- cyclopropyl)propionic acid, new methano-l-lysines, is described. The synthetic route includes nine steps from l-methionine, with a key step involving the cyclopropanation of an intermediate E-allylic alcohol. The resultant hydroxymethylcyclopropanes were readily separated and converted into the title α-amino acids. The stereochemistry around the cyclopropane rings was deduced by conducting the cyclopropanation in the presence of N,N,N′,N′-tetramethyl-d-tartaric acid diamide butylboronate, a chiral controller which is known to favour the production of S-hydroxymethyl cyclopropanes from allylic alcohols.