2895-21-8Relevant articles and documents
Chirality sensing and size discrimination of anions by macrotricyclic cyclen-disodium complexes
Ito, Hiroshi,Shinoda, Satoshi
, p. 238 - 241 (2014)
Two macrotricyclic ligands composed of two face-to-face octadentate metal chelates were synthesized. These cage-shaped disodium complexes had special recognition ability for various counter anions. Specific chiral dicarboxylates bound to the complexes within the cavity and exhibited chirality induction properties. For instance, N-Boc-Asp dianion strongly induced circular dichroism (CD) signals, but N-Boc-Glu dianion, which is one carbon longer, did not. Chirality on Na+: The first example of chirality sensing on Na+ was achieved by a macrotricyclic host composed of two octadentate cyclen-Na+ complexes. Chiral N-Boc-Asp dianions coordinated to the Na+ at the cavity, resulting in the chirality induction of the cage molecule, but N-Boc-Glu dianion, which is one carbon longer, did not.
4-Arylthieno[2,3-b]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents
Alder, Arne,Gilberger, Tim,Kunick, Conrad,Schwed, Sandra I.
, (2020/08/24)
Malaria causes hundreds of thousands of deaths every year, making it one of the most dangerous infectious diseases worldwide. Because the pathogens have developed resistance against most of the established anti-malarial drugs, new antiplasmodial agents are urgently needed. In analogy to similar antiplasmodial ketones, 4-arylthieno[2,3-b]pyridine-2-carboxamides were synthesized by Thorpe-Ziegler reactions. In contrast to the related ketones, these carboxamides are only weak inhibitors of the plasmodial enzyme PfGSK-3 but the compounds nevertheless show strong antiparasitic activity. The most potent representatives inhibit the pathogens with IC50values in the two-digit nanomolar range and exhibit high selectivity indices (>100).
GLUCOSE UPTAKE INHIBITORS
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Paragraph 0196; 0199-0201, (2020/01/24)
this invention provides compounds that modulate glucose uptake activity and cellular transport/uptake of glucose, and particularly GLUTS3, but also including but not limited to GLUT1-14 (SLC2A1-SLC2A14). Compounds of the invention are useful for treating diseases, including cancer, autoimmune diseases and inflammation, infectious diseases, and metabolic diseases.