- Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti-malaria Activity in Humanized Mice
-
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
- 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)
-
- PROCESS FOR THE PREPARATION OF N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE
-
The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employ
- -
-
Page/Page column 28; 29; 30; 31; 32
(2019/02/06)
-
- MACROCYCLIC COMPOUNDS AS PROTEASOME INHIBITORS
-
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.
- -
-
-
- CYCLOBUTANE- AND AZETIDINE-CONTAINING MONO AND SPIROCYCLIC COMPOUNDS AS ALPHA V INTEGRIN INHIBITORS
-
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αv- containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of av-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
- -
-
-
- 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
-
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.
- 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 facile transformation of amino acids to functionalized coumarins
-
The synthesis of novel chiral coumarins functionalized with proteinogenic amino acid side chains via N-protected γ-amino-β-keto esters and their incorporation into the cell permeable HIV-1 TAT peptide through the modified solid phase peptide synthesis are
- Bandyopadhyay, Anupam,Gopi, Hosahudya N.
-
p. 8089 - 8095
(2012/01/04)
-
- Synthesis of a serine-based neuraminic acid C-glycoside
-
Cell-surface carbohydrates are classified by the nature of their linkages to the protein as either N-linked or O-linked. O- and N-glycans are involved in a number of important biological functions. These activities can be lost on glycoprotein catabolism w
- Wang, Qun,Linhardt, Robert J.
-
p. 2668 - 2672
(2007/10/03)
-
- 4-N-Hydroxy-L-2,4-diaminobutyric acid. A strong inhibitor of glutamine synthetase
-
Analogues of glutamic acid were synthesized and evaluated for their inhibitory activity toward glutamine synthetase (EC 6.3.1.2; GS). The title compound, 4-N-hydroxy-L-2,4-diaminobutyric acid (NH-DABA), showed a potent inhibitory activity against GS from
- Fushiya,Maeda,Funayama,Nozoe
-
p. 480 - 483
(2007/10/02)
-