Design and synthesis of novel antimicrobials

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 409/02 (2006.01) A61K 31/41 (2006.01) A61P 31/00 (2006.01) A61P 31/04 (2006.01) C07D 409/04 (2006.01) C12Q 1/00 (2006.01)

Patent

CA 2603534

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 Pl, 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.

L'invention concerne la synthèse de nouveaux inhibiteurs de LpxA et leur activité. Ces composés sont conçus sur un modèle de récepteur développé à l'aide de la structure cristalline de LpxA, et sont agencés pour présenter une interaction de liaison favorable sur le site actif de cette enzyme.

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