Tetrahydropyridine derivatives as FabI inhibitors

摘要

The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors.;
in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity.
;The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

主权项

1. A compound of formula (1)or a pharmaceutically acceptable salt or a pharmaceutically acceptable stereoisomer thereof,wherein,
X represents N or CH; Y represents NR1 or CHR1; Z represents CR2R3; R1 represents hydrogen or alkyl; R2 and R3 are independently selected from hydrogen and alkyl; alternatively, R2 and R3 may be taken together with the carbon atoms to which they are attached to form an optionally substituted 3-7 membered ring containing 0-3 hetero atoms or groups; wherein the optional substituent is R4 and the heteroatoms are independently selected from N, O, NH and CO in any stable combination; alternatively, R1 and R2 may be taken together with the carbon or nitrogen atom to which they are attached to form 5-membered fused ring; R4 at each occurrence is selected from alkyl, —COOR5, —COR5, —CONR5R5, —SO2R5, —COCH2OR5, —CO(CH2)2COOR5, —COCH2NR5R5 and cycloalkyl; R5 at each occurrence is selected from hydrogen, alkyl, cycloalkyl and heterocyclyl; and ‘n’ is selected from an integer 0 or 1.