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Pentafluorosulfanyl as a Novel Building Block for Enzyme Inhibitors: Trypanothione Reductase Inhibition and Antiprotozoal Activities of Diarylamines
Author(s) -
Stump Bernhard,
Eberle Christian,
Schweizer W. Bernd,
Kaiser Marcel,
Brun Reto,
KrauthSiegel R. Luise,
Lentz Dieter,
Diederich François
Publication year - 2009
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200800565
Subject(s) - chemistry , enzyme , antiprotozoal , substituent , biochemistry , in vitro , stereochemistry , pharmacology , biology
Pentafluorosulfanyl power! The SF 5 group—a novel substituent with striking physicochemical properties—was used as building block for trypanothione reductase (TR) inhibitors and compared to its CF 3 and C(CH 3 ) 3 relatives. The high in vitro activities of these derivatives against Trypanosoma brucei rhodesiense as well as against Plasmodium falciparum supports the suitability of SF 5 as a component of drug‐like compounds.