Structure-activity analysis of CJ-15,801 analogues that interact with Plasmodium falciparum pantothenate kinase and inhibit parasite proliferation

2018 ◽  
Vol 143 ◽  
pp. 1139-1147 ◽  
Author(s):  
Christina Spry ◽  
Alan L. Sewell ◽  
Yuliya Hering ◽  
Mathew V.J. Villa ◽  
Jonas Weber ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Activity Analysis ◽  
Pantothenate Kinase ◽  
Structure Activity

scholarly journals Antiplasmodial Chalcones Inhibit Sorbitol-Induced Hemolysis of Plasmodium falciparum-Infected Erythrocytes

2004 ◽  
Vol 48 (9) ◽  
pp. 3241-3245 ◽  
Author(s):  
Mei-Lin Go ◽  
Mei Liu ◽  
Prapon Wilairat ◽  
Philip J. Rosenthal ◽  
Kevin J. Saliba ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Erythrocyte Membrane ◽  
Malaria Parasite ◽  
Important Determinant ◽  
Activity Analysis ◽  
Significant Extent ◽  
Active Compounds ◽  
Structure Activity ◽  
Qualitative Structure

ABSTRACT A series of alkoxylated and hydroxylated chalcones previously reported to have antiplasmodial activities in vitro were investigated for their effects on the new permeation pathways induced by the malaria parasite in the host erythrocyte membrane. Of 21 compounds with good antiplasmodial activities (50% inhibitory concentrations [IC50s], ≤20 μM), 8 members were found to inhibit sorbitol-induced lysis of parasitized erythrocytes to a significant extent (≤40% of control values) at a concentration (10 μM) that was close to their antiplasmodial IC50s. Qualitative structure-activity analysis suggested that activity was governed to a greater extent by a substitution on ring B than on ring A of the chalcone template. Most of the active compounds had methoxy or dimethoxy groups on ring B. Considerable variety was permitted on ring A in terms of the electron-donating or -withdrawing property. Lipophilicity did not appear to be an important determinant for activity. Although they are not exceptionally potent as inhibitors (lowest IC50, 1.9 μM), the chalcones compare favorably with other more potent inhibitors in terms of their selective toxicities against plasmodia and their neutral character.

A Structure–Activity Analysis of Biased Agonism at the Dopamine D2 Receptor

2013 ◽  
Vol 56 (22) ◽  
pp. 9199-9221 ◽  
Author(s):  
Jeremy Shonberg ◽  
Carmen Klein Herenbrink ◽  
Laura López ◽  
Arthur Christopoulos ◽  
Peter J. Scammells ◽  
...  
Keyword(s):  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Activity Analysis ◽  
Biased Agonism ◽  
Dopamine D2 ◽  
Structure Activity

scholarly journals Clinanthus microstephium , an Amaryllidaceae Species with Cholinesterase Inhibitor Alkaloids: Structure−Activity Analysis of Haemanthamine Skeleton Derivatives

2019 ◽  
Vol 16 (5) ◽  
pp. e1800662
Author(s):  
Tonino G. Adessi ◽  
José L. Borioni ◽  
Natalia B. Pigni ◽  
Jaume Bastida ◽  
Valeria Cavallaro ◽  
...  
Keyword(s):  
Cholinesterase Inhibitor ◽  
Activity Analysis ◽  
Structure Activity
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