title: Pyrrolidinedione derivatives as antibacterial agents with a novel mode of action.
abstract: The pseudopeptide pyrrolidinedione natural products moiramide B and andrimid represent a new class of antibiotics that target bacterial fatty acid biosynthesis. Structure-activity relationship (SAR) studies revealed a high degree of variability for the fatty acid side chain, allowing optimization of physicochemical parameters, and a restricted SAR for the pyrrolidinedione group, indicating major relevance of this subunit for efficient target binding.
authors.affiliation: Department of Medicinal Chemistry, Bayer HealthCare AG, D-42096 Wuppertal, Germany.
authors.forename: Jens
authors.initials: J
authors.lastname: Pohlmann
authors.forename: Thomas
authors.initials: T
authors.lastname: Lampe
authors.forename: Mitsuyuki
authors.initials: M
authors.lastname: Shimada
authors.forename: Peter G
authors.initials: PG
authors.lastname: Nell
authors.forename: Josef
authors.initials: J
authors.lastname: Pernerstorfer
authors.forename: Niels
authors.initials: N
authors.lastname: Svenstrup
authors.forename: Nina A
authors.initials: NA
authors.lastname: Brunner
authors.forename: Guido
authors.initials: G
authors.lastname: Schiffer
authors.forename: Christoph
authors.initials: C
authors.lastname: Freiberg
mesh_terms: D000103:Acetyl-CoA Carboxylase / Q000037:antagonists & inhibitors; D000577:Amides; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D005227:Fatty Acids / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D008826:Microbial Sensitivity Tests; D011090:Polyenes; D011758:Pyrroles; D013329:Structure-Activity Relationship; D013388:Succinimides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000577:Amides; D000900:Anti-Bacterial Agents; D005227:Fatty Acids; D011090:Polyenes; D011758:Pyrroles; D013388:Succinimides; C487819:moiramide B; C088069:andrimid; D000103:Acetyl-CoA Carboxylase