Novel nitrophenylaziridine compounds and their use as prodrugs

Details Novel nitrophenylaziridine compounds and their use as prodrugs Novel nitrophenylaziridine compounds and their use as prodrugs

A - Human Necessities

61

K

A61K 31/395 (2006.01) A61K 31/396 (2006.01) A61K 31/415 (2006.01) A61K 31/4178 (2006.01) A61K 31/535 (2006.01) A61K 31/5377 (2006.01) C07D 203/08 (2006.01) C07D 203/14 (2006.01) C07D 403/12 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2342943

A range of aziridin-1-yl nitrobenzamides (A-C) are provided for use as prodrugs in conjunction with nitroreductase (NR) enzymes. The amides may have 1 or 2 N-substituents which may be bulky and polar. For example, 5-(aziridin-1- yl) -N-[2-(4-morpholino) ethyl] -2,4-dinitrobenzamide of Compound (1) was found to be highly active against all NR+ cell lines tested.

L'invention porte sur une gamme d'aziridin-1-Yl nitrobenzamides utilisés comme prodrogues en association avec des enzymes du type nitroréductase (NR). Lesdits amides peuvent comporter 1 ou 2 substituants massifs ou polaires. Il peut par exemple s'agir du 5-(aziridin-1-Yl) N-[2-(4-morpholino)éthyl] -2,4-dinitrobenzamide du composant (1) qui s'est avéré très actif contre toutes les lignées de cellules NR+ testées.

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