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Inside Cover: Synthesis, Inhibition Potency, Binding Mode, and Antiprotozoal Activities of Fluorescent Inhibitors of Trypanothione Reductase Based on Mepacrine‐Conjugated Diaryl Sulfide Scaffolds (ChemMedChem 12/2009)
Author(s) -
Eberle Christian,
Burkhard Johannes A.,
Stump Bernhard,
Kaiser Marcel,
Brun Reto,
KrauthSiegel R. Luise,
Diederich François
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200990057
Subject(s) - chemistry , fluorescence , potency , conjugated system , antiprotozoal , enzyme , non competitive inhibition , stereochemistry , biochemistry , mode of action , combinatorial chemistry , in vitro , organic chemistry , physics , quantum mechanics , polymer
The inside cover picture shows a modeled structure of a novel competitive inhibitor of trypanothione reductase (TR) in the active site of the enzyme. TR is unique to trypanosomatid parasites and a target for lead discovery programs. The parasites depicted show the high accumulation of the fluorescent inhibitors in T. b. rhodesiense. For more details, see the Full Paper by F. Diederich et al. on p. 2034 ff.