N-formyl hydroxylamine compounds as pdf inhibitors

Details N-formyl hydroxylamine compounds as pdf inhibitors N-formyl hydroxylamine compounds as pdf inhibitors

C - Chemistry, Metallurgy

07

D

C07D 403/12 (2006.01) A61P 31/04 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2608634

Novel N-formyl hydroxylamine compounds (I) and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes . The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed. wherein R1 is hydrogen, alkyl, heteroalkyi, heterocycloalkyl, aryl or heteroaryl.; R3 is hydrogen, halogen, or alkoxy; R4 is aryl, or heteroaryl; or n is 0 to 3 and provided that R1 is cycloalkyl and/or R4 is an optionally substituted 6 membered, monocyclic heteroaryl ring having 2, 3 or 4 nitrogen heteroatoms in the ring wherein one or more of the ring nitrogen heteroatoms is optionally oxidized.

L'invention concerne des nouveaux composés de N-formylhydroxylamine et leurs dérivés. Ces composés de N-formylhydroxylamine inhibent la peptidyle déformylase (PDF), une enzyme présente dans les procaryotes. Ces composés sont utiles en tant qu'antimicrobiens et qu'antibiotiques. Les composés de l'invention présentent une inhibition sélective de la peptidyle déformylase contre d'autres métalloprotéinases de type MMP. L'invention concerne également des méthodes de préparation et d'utilisation desdits composés.

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