2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound

Details 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound

C - Chemistry, Metallurgy

07

D

C07D 498/04 (2006.01) A61K 31/424 (2006.01) A61K 31/4245 (2006.01) A61K 31/428 (2006.01) A61K 31/438 (2006.01) A61K 31/4439 (2006.01) A61K 31/454 (2006.01) A61K 31/4545 (2006.01) A61K 31/46 (2006.01) A61K 31/4709 (2006.01) A61K 31/4725 (2006.01) A61K 31/496 (2006.01) A61K 31/497 (2006.01) A61K 31/498 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61K 31/551 (2006.01) A61K 31/695 (2006.01) A61P 31/06 (2006.01) C07D 498/20 (2006.01) C07D 519/00 (2006.01) C07F 7/08 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2497569

The present invention provides a 2,3-dihydro- 6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (see formula 1) wherein R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R2 represents a group -OR3 or the like, and R3 represents a hydrogen atom, C1-C6 alkyl group or the like, or R1 and -(CH2)n R2 may bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H): (see formula H) wherein R41 is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.

L'invention concerne des 2,3-dihydro-6-nitroimidazo[2,1-b]oxazoles représentés par la formule générale (1), dans laquelle R?1¿ est un atome d'hydrogène ou un groupe alkyle C¿1-6?, n est un nombre entier compris entre 0 et 6 et R?2¿ est un groupe OR?3¿ ou similaire, R?3¿ représentant un atome d'hydrogène, un groupe alkyle C¿1-6? ou similaire, ou R?1¿ et (CH¿2?)¿n?R?2¿ peuvent être unis par un atome d'azote pour former avec l'atome de carbone adjacent un cycle spiro représenté par la formule générale (H), dans laquelle R?41¿ est un atome d'hydrogène, un groupe alkyle C¿1-6? ou similaire. Les composés selon l'invention présentent une excellente activité bactéricide contre le bacille tuberculeux, le bacille tuberculeux résistant à de multiples médicaments et les bactéries acido-résistantes atypiques.

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