5-amidomethyl .alpha.,.beta.-saturated and -unsaturated 3-aryl b

Details 5-amidomethyl .alpha.,.beta.-saturated and -unsaturated 3-aryl b 5-amidomethyl .alpha.,.beta.-saturated and -unsaturated 3-aryl b

1996-09-05

1998-01-13

Dentz, Bernard

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540362, 540363, 540950, 544 47, 544 60, 544105, 546214, 548255, 5482644, 5483154, 5483641, 548453, 548466, 548469, 548517, 549321, C07D41310, C07D30758, C07D30733

Patent

active

057081697

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, 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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