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2005
Pyrrole derivatives
R 0120
Pyrrolidinedione Derivatives as Antibacterial Agents with a Novel Mode of
— Variations of the two terminal subunits of the natural products moiramide
26- 062 Action.
B and andrimid, the fatty acid side chain and the pyrrolidinedione group, are explored.
All compounds are tested for target activity against the carboxytransferase AccAD subunits derived from S. aureus and E. coli, representing Gram-positive and Gram-negative pathogens. Antibacterial activity is measured vs. S. aureus and S. pneumoniae as
Gram-positive bacteria, and vs. two E. coli strains. Variations of the fatty acid side chain
show that quite diverse substituents are tolerated, cf. (VII). Despite limited influence
on enzyme inhibition, a significant impact on antibacterial activity is observed. In contrast to the broad variations tolerated at the fatty acid side chain, only limited variations
are tolerated in the pyrrolidinedione head group, cf. (VIII). — (POHLMANN, J.;
LAMPE, T.; SHIMADA, M.; NELL, P. G.; PERNERSTORFER, J.; SVENSTRUP, N.;
BRUNNER, N. A.; SCHIFFER, G.; FREIBERG*, C.; Bioorg. Med. Chem. Lett. 15
(2005) 4, 1189-1192; Dep. Anti-Infect. Res., Bayer HealthCare AG,
D-42096 Wuppertal, Germany; Eng.) — H. Hoennerscheid
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