Novel 1,4-benzodiazepines, endowed with a Michael acceptor moiety, were designed taking advantage ofa computational prediction of their pharmacokinetic parameters. Among all the synthesized derivatives,we identified a new lead compound (i.e.,4a), bearing a vinyl ketone warhead and endowed with apromising antitrypanosomal activity againstTrypanosoma brucei brucei(IC50= 5.29lM), coupled with alack of cytotoxicity towards mammalian cells (TC50>100lM).
Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents
ETTARI, RobertaPrimo
;PREVITI, SANTO;MAIORANA, SANTINA;GRASSO, Silvana;ZAPPALA', Maria
Ultimo
2016-01-01
Abstract
Novel 1,4-benzodiazepines, endowed with a Michael acceptor moiety, were designed taking advantage ofa computational prediction of their pharmacokinetic parameters. Among all the synthesized derivatives,we identified a new lead compound (i.e.,4a), bearing a vinyl ketone warhead and endowed with apromising antitrypanosomal activity againstTrypanosoma brucei brucei(IC50= 5.29lM), coupled with alack of cytotoxicity towards mammalian cells (TC50>100lM).File in questo prodotto:
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