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5 amide methyl , saturation and unsaturated 3 aryl butyrolactone anti-bacterial medicine
5 amide methyl , saturation and unsaturated 3 aryl butyrolactone anti-bacterial medicine
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机译:5酰胺甲基,饱和和不饱和3芳基丁内酯抗菌药
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摘要
The present invention provides for new 5-amidomethyl, alpha , beta -saturated and-unsaturated butyrolactone antibacterial agents of formula I IMAGE I characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substituted with zero (0) to two(2) halogen atoms and substituted in the para position with, e.g., piperazinyl, thiomorpholinyl (and corresponding sulfoxide and sulfone), thiazolidinyl (and sulfoxide and sulfone), morpholinyl, azetidinyl, pyrrolidinyl, piperidinyl, pyrrolyl, azepinyl, troponyl, 3,7-diazabicyclo[3.3.0]octan-3-yl, bridged thiazinyl or bridged oxazinyl moieties. In those cases where a ring nitrogen is present, then this is substituted to form an amide, formamide, sulfonamide, urethane, or alkylated with a wide variety of moieties. These compounds are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci, as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.
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