title: 4-Aminothiazolyl analogues of GE2270 A: antibacterial lead finding.
abstract: 4-Aminothiazolyl analogues of the antibacterial natural product GE2270 A (1) were designed, synthesized, and evaluated for gram positive bacteria growth inhibition. The aminothiazole-based chemical template was evaluated for chemical stability, and its decomposition revealed a novel, structurally simplified, des-thiazole analogue of 1. Subsequent stabilization of the 4-aminothiazolyl functional motif was achieved and initial structure activity relationships defined.
authors.affiliation: Global Discovery Chemistry, Novartis Institutes for Biomedical Research, Cambridge, Massachusetts 02139, United States. matthew.lamarche@novartis.com
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: LaMarche
authors.forename: Jennifer A
authors.initials: JA
authors.lastname: Leeds
authors.forename: JoAnne
authors.initials: J
authors.lastname: Dzink-Fox
authors.forename: Karl
authors.initials: K
authors.lastname: Gunderson
authors.forename: Philipp
authors.initials: P
authors.lastname: Krastel
authors.forename: Klaus
authors.initials: K
authors.lastname: Memmert
authors.forename: Michael A
authors.initials: MA
authors.lastname: Patane
authors.forename: Elin M
authors.initials: EM
authors.lastname: Rann
authors.forename: Esther
authors.initials: E
authors.lastname: Schmitt
authors.forename: Stacey
authors.initials: S
authors.lastname: Tiamfook
authors.forename: Bing
authors.initials: B
authors.lastname: Wang
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D055808:Drug Discovery; D004355:Drug Stability; D008826:Microbial Sensitivity Tests; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D010456:Peptides, Cyclic; D013844:Thiazoles; C068122:GE 2270 A