title: Preparation of novel antibacterial agents. Replacement of the central aromatic ring with heterocycles.
abstract: Discovery of novel antibacterial agents is a significant challenge. We have recently reported on our discovery of novel antibacterial agents in which we have rapidly optimized potency utilizing a parallel chemistry approach. These advanced leads suffer from high affinity for human serum albumin (HSA). In an effort to decrease the affinity for HSA we have prepared a series of heterocyclic analogs, which retained antibacterial activity and demonstrated reduced affinity for HSA.
authors.affiliation: Medicinal Chemistry and Infectious Diseases Biology, Pharmacia Corporation, 301 Henrietta Street, Kalamazoo, MI 49001, USA.
authors.forename: Jianke
authors.initials: J
authors.lastname: Li
authors.forename: Brian D
authors.initials: BD
authors.lastname: Wakefield
authors.forename: J Craig
authors.initials: JC
authors.lastname: Ruble
authors.forename: Cory M
authors.initials: CM
authors.lastname: Stiff
authors.forename: Donna L
authors.initials: DL
authors.lastname: Romero
authors.forename: Keith R
authors.initials: KR
authors.lastname: Marotti
authors.forename: Michael T
authors.initials: MT
authors.lastname: Sweeney
authors.forename: Gary E
authors.initials: GE
authors.lastname: Zurenko
authors.forename: Douglas C
authors.initials: DC
authors.lastname: Rohrer
authors.forename: Atli
authors.initials: A
authors.lastname: Thorarensen
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D001419:Bacteria / Q000187:drug effects; D006571:Heterocyclic Compounds; D006801:Humans; D008826:Microbial Sensitivity Tests; D011485:Protein Binding; D012709:Serum Albumin / Q000378:metabolism; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates
chemical_list: D000900:Anti-Bacterial Agents; D006571:Heterocyclic Compounds; D012709:Serum Albumin; D062367:ortho-Aminobenzoates; C031385:anthranilic acid