- Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin
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High-throughput screening has shown that Retro-1 inhibits ricin and Shiga toxins by diminishing their intracellular trafficking via the retrograde route, from early endosomes to the Golgi apparatus. To improve the activity of Retro-1, a structure-activity relationship (SAR) study was undertaken and yielded an analogue with a roughly 70-fold better half-maximal effective concentration (EC50) against Shiga toxin cytotoxicity measured in a cell protein synthesis assay.
- Abdelkafi, Hajer,Michau, Aurélien,Pons, Valérie,Ngadjeua, Flora,Clerget, Alexandra,Ait Ouarab, Lilia,Buisson, David-Alexandre,Montoir, David,Caramelle, Lucie,Gillet, Daniel,Barbier, Julien,Cintrat, Jean-Christophe
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p. 8114 - 8133
(2020/09/21)
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- Amide-Based Cinchona Alkaloids as Phase-Transfer Catalysts: Synthesis and Potential Application
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Herein we present a library of simple amide derivatives of Cinchona alkaloids in the form of quaternary ammonium salts. The obtained derivatives can be generated very easily and efficiently from inexpensive and commercially available substrates. We tested this class of alkaloids in the alkylation of glycine derivative, carried out under phase-transfer catalyst conditions. The presented hybrid catalysts offer both high reaction yields (up to 97%) and high enantioselectivities of the obtained product (up to 94% ee).
- Majdecki, Maciej,Niedbala, Patryk,Jurczak, Janusz
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supporting information
p. 8085 - 8090
(2019/10/14)
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- Axially chiral Ni(II) complexes of α-amino acids: Separation of enantiomers and kinetics of racemization
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Herein we present design, synthesis, chiral HPLC resolution, and kinetics of racemization of axially chiral Ni(II) complexes of glycine and di-(benzyl)glycine Schiff bases. We found that while the ortho-fluoro derivatives are configurationally unstable, t
- Zhang, Wenzhong,Ekomo, Romuald Eto,Roussel, Christian,Moriwaki, Hiroki,Abe, Hidenori,Han, Jianlin,Soloshonok, Vadim A.
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p. 498 - 508
(2018/01/27)
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- Synthesis and spectral properties of 2-[(o- and p-substituted)aminophenyl]-3H-5-[(o- and p-substituted)phenyl]-7-chloro-1,4-benzodiazepines
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A series of twelve new 2-[(o- and p-substituted)aminophenyl]-3H-5-[(o- and p-substituted)phenyl]-7-chloro-1,4-benzodiazepines, which have possible pharmacological properties has been obtained. The synthesis was carried out following six steps. The structure of all products was corroborated by ir, 1H nmr, 13C nmr and ms. In addition for the compound 2-(o-chloroaminophenyl)-3H-5-(o-fluorophenyl)-7-chloro-1,4-benzodiazepine 7, its structure was confirmed by X-ray diffraction.
- Cortes Cortes,Salazar Franco,Garcia Mellado
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p. 663 - 669
(2007/10/03)
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