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    5-amidomethyl .alpha.,.beta.-saturated and -unsaturated 3-aryl butyrolactone antibacterial agents
    7.
    发明授权
    5-amidomethyl .alpha.,.beta.-saturated and -unsaturated 3-aryl butyrolactone antibacterial agents 失效
    5-酰氨基甲基α，β-饱和和不饱和3-芳基丁内酯抗菌剂

    公开(公告)号：US5708169A

    公开(公告)日：1998-01-13

    申请号：US708765

    申请日：1996-09-05

    Applicant: Jackson B. Hester, Jr. ,  Steven Joseph Brickner ,  Michael Robert Barbachyn ,  Douglas K. Hutchinson ,  Dana Scott Toops

    Inventor： Jackson B. Hester, Jr. ,  Steven Joseph Brickner ,  Michael Robert Barbachyn ,  Douglas K. Hutchinson ,  Dana Scott Toops

    IPC: C07D307/58 ,  A61K31/00 ,  A61K31/34 ,  A61K31/341 ,  A61P31/00 ,  A61P31/04 ,  C07D307/28 ,  C07D307/52 ,  C07D413/10 ,  C07D307/33

    CPC classification number: C07D307/58 ,  C07D307/28 ,  C07D307/52

    Abstract: The present invention provides for new 5-amidomethyl, .alpha.,.beta.-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## 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.

    Abstract translation: 本发明提供式I的新的5-氨基甲基，α，β饱和和不饱和丁内酯抗菌剂，其特征在于3-芳基取代基，包括例如二氢吲哚基和被0（0）至 二（2）个卤素原子并且在对位置被例如哌嗪基，硫代吗啉基（和相应的亚砜和砜），噻唑烷基（和亚砜和砜），吗啉基，氮杂环丁烷基，吡咯烷基，哌啶基，吡咯基，氮杂基， ，7-二氮杂双环[3.3.0]辛-3-基，桥连噻嗪基或桥连的恶嗪基部分。 在存在环状氮的情况下，将其取代形成酰胺，甲酰胺，磺酰胺，氨基甲酸酯或用各种部分烷基化。 这些化合物对许多人类和兽医病原体有效，包括革兰氏阳性需氧细菌，如耐多发性葡萄球菌，链球菌和肠球菌，以及厌氧生物体如拟杆菌属。 和梭菌属（Clostridia spp。） 物种和耐酸生物，如结核分枝杆菌，鸟分枝杆菌和分枝杆菌，以及生物体如支原体属（Mycoplasma spp）。

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