The invention relates to compds. of formula I, pharmaceutical compns. comprising these compds., their use in the treatment of kinetoplastid infections and their prepn. Compds. of formula I, wherein A is absent, O, S, etc.; B is absent, (CH2)​n and CO; Z is absent, CO, SO2, etc.; X and Y are independently H, halo, C1-​6 alkyl, etc.; m and n are 1 or 2 wherein at least one must be 1; p is 0 , 1 and 2; Het is 1H-​imidazole, 4H-​1,​2,​4-​triazole, oxazole, etc.; R1 is naphthalen-​2-​yl, 2-​methoxyquinolin-​3-​yl, pryimdin-​5-​yl, etc.; R2 is H, C6-​10 aryl, C3-​15 heterocyclyl, etc.; and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, are claimed. Compd. II.bul.TFA was prepd. using a multistep procedure (procedure given)​. Compds. of the invention were tested for their inhibitory activity against T. brucei (data given)​.

Heterocyclic compounds used in the treatment of kinetoplastid infection and their preparation / Biancofiore, Ilaria; Ciammaichella, Alina; Ferrigno, Federica; Harper, Steven; Malancona, Savina; Ontoria Ontoria, Jesus Maria; Paonessa, Giacomo; Ponzi, Simona; Summa, Vincenzo. - (2017).

Heterocyclic compounds used in the treatment of kinetoplastid infection and their preparation

Summa, Vincenzo
2017

Abstract

The invention relates to compds. of formula I, pharmaceutical compns. comprising these compds., their use in the treatment of kinetoplastid infections and their prepn. Compds. of formula I, wherein A is absent, O, S, etc.; B is absent, (CH2)​n and CO; Z is absent, CO, SO2, etc.; X and Y are independently H, halo, C1-​6 alkyl, etc.; m and n are 1 or 2 wherein at least one must be 1; p is 0 , 1 and 2; Het is 1H-​imidazole, 4H-​1,​2,​4-​triazole, oxazole, etc.; R1 is naphthalen-​2-​yl, 2-​methoxyquinolin-​3-​yl, pryimdin-​5-​yl, etc.; R2 is H, C6-​10 aryl, C3-​15 heterocyclyl, etc.; and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, are claimed. Compd. II.bul.TFA was prepd. using a multistep procedure (procedure given)​. Compds. of the invention were tested for their inhibitory activity against T. brucei (data given)​.
2017
Heterocyclic compounds used in the treatment of kinetoplastid infection and their preparation / Biancofiore, Ilaria; Ciammaichella, Alina; Ferrigno, Federica; Harper, Steven; Malancona, Savina; Ontoria Ontoria, Jesus Maria; Paonessa, Giacomo; Ponzi, Simona; Summa, Vincenzo. - (2017).
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/828332
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