20266-00-6Relevant articles and documents
Dialkylaminoalkyl derivatives of bicyclic compounds with antiplasmodial activity
Faist, Johanna,Seebacher, Werner,Kaiser, Marcel,Brun, Reto,Saf, Robert,Weis, Robert
, p. 6796 - 6804 (2010)
Dialkylaminoalkyl derivatives of 2-azabicyclo[3.2.2]nonanes and of bicyclo[2.2.2]octanes were prepared and their activities determined in vitro against the multiresistant K1 strain of Plasmodium falciparum. Several of the new compounds exhibited very promising antiplasmodial activity and selectivity. The results were compared to those of formerly synthesized analogues and of drugs in use. Structure-activity relationships were detected. Some of the more potent compounds were tested in vivo against Plasmodium berghei showing weak to moderate activity. A single compound was able to increase the mean survival days of infected mice.
Microwave-assisted synthesis, structural characterization and assessment of the antibacterial activity of some new aminopyridine, pyrrolidine, piperidine and morpholine acetamides
Abdulghani, Saba S.,Alsamarrai, Abdulmajeed S. H.
, (2021/06/14)
A series of new acetamide derivatives 22–28 of primary and secondary amines and para-toluene sulphinate sodium salt have been synthesized under microwave irradiation and assessed in vitro for their antibacterial activity against one Gram-positive and two Gram-negative bacterial species such as S. pyogenes, E. coli, and P. mirabilis using the Mueller-Hinton Agar diffusion (well diffusion) method. The synthesized compounds with significant differences in inhibition diameters and MICs were compared with those of amoxicillin, ampicillin, cephalothin, azithromycin and doxycycline. All of the evaluated acetamide derivatives were used with varying inhibition concentrations of 6.25, 12.5, 37.5, 62.5, 87.5, 112.5 and 125 μg/mL. The results show that the most important antibacterial properties were displayed by the synthetic compounds 22 and 24, both of bear a para-chlorophenyl moiety incorporated into the 2-position moiety of acetamide 1. The molecular structures of the new compounds were determined using the FT-IR and1H-NMR techniques.
COMPOUNDS FOR USE IN TREATING NEUROLOGICAL DISORDERS
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Paragraph 00196-00197, (2021/02/05)
Provided are methods for treating neurological disorders using compounds of Formula (I), and pharmaceutically acceptable salts and compositions thereof.
Discovery and Optimization of Glucose Uptake Inhibitors
Liu, Kevin G.,Kim, Ji-In,Olszewski, Kellen,Barsotti, Anthony M.,Morris, Koi,Lamarque, Christophe,Yu, Xuemei,Gaffney, Jack,Feng, Xiao-Jiang,Patel, Jeegar P.,Poyurovsky, Masha V.
supporting information, p. 5201 - 5211 (2020/07/10)
Aerobic glycolysis, originally identified by Warburg as a hallmark of cancer, has recently been implicated in immune cell activation and growth. Glucose, the starting material for glycolysis, is transported through the cellular membrane by a family of glucose transporters (GLUTs). Therefore, targeting glucose transporters to regulate aerobic glycolysis is an attractive approach to identify potential therapeutic agents for cancers and autoimmune diseases. Herein, we describe the discovery and optimization of a class of potent, orally bioavailable inhibitors of glucose transporters, targeting both GLUT1 and GLUT3.
