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, Roberta
Primo
;
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).
2016
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11570/3089054
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