101620-09-1Relevant articles and documents
Synthesis, Structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds
Burgess, Steven J.,Kelly, Jane X.,Shomloo, Shawheen,Wittlin, Sergio,Brun, Reto,Liebmann, Katherine,Peyton, David H.
experimental part, p. 6477 - 6489 (2010/11/05)
We have previously shown that a "reversed chloroquine (RCQ)" molecule, composed of a chloroquine-like moiety and a resistance reversal-like moiety, can overcome chloroquine resistance in P. falciparum (Burgess, S. J.; Selzer, A.; Kelly, J. X.; Smilkstein, M. J.; Riscoe, M. K.; Peyton, D. H. J. Med. Chem. 2006, 49, 5623. Andrews, S.; Burgess, S. J.; Skaalrud, D.; Kelly, J. X.; Peyton, D. H. J. Med. Chem. 2010, 53, 916). Here, we present an investigation into the Structure-activity relationship of the RCQ structures, resulting in an orally active molecule with good in vitro and in vivo antimalarial activity. We also present evidence of the mode of action, indicating that the RCQ molecules inhibit hemozoin formation in the parasite's digestive vacuole in a manner similar to that of chloroquine.
THIAZOLIDINECARBOXYLIC ACID AMIDE DERIVATIVES AND THEIR THERAPEUTIC USES
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, (2008/06/13)
Thiazolidinecarboxylic acid amides having combined antiallergic and antiasthmatic activities with an antagonist activity against platelet Activating Factor and having the following general formula (I) STR1