Synthesis of novel antimicrobials

摘要

The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.

主权项

1. A method of inhibiting growth of a bacterium selected from the group consisting of Escherichia coli, Enterococcus faecalis and Staphylococcus aureus to treat a bacterial infection caused by said bacterium, said method comprising administering to an individual in need of such treatment, an effective amount of a purified compound having the structure:wherein ‘(Hal)’ is any halogen, or a pharmaceutically acceptable salt thereof.