title: Potent inhibitors of LpxC for the treatment of Gram-negative infections.
abstract: In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel series of potent antibacterial LpxC inhibitors represented by hydroxamic acid.
authors.affiliation: Worldwide Medicinal Chemistry, Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States. matthew.f.brown@pfizer.com
authors.forename: Matthew F
authors.initials: MF
authors.lastname: Brown
authors.forename: Usa
authors.initials: U
authors.lastname: Reilly
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Abramite
authors.forename: Joel T
authors.initials: JT
authors.lastname: Arcari
authors.forename: Robert
authors.initials: R
authors.lastname: Oliver
authors.forename: Rose A
authors.initials: RA
authors.lastname: Barham
authors.forename: Ye
authors.initials: Y
authors.lastname: Che
authors.forename: Jinshan Michael
authors.initials: JM
authors.lastname: Chen
authors.forename: Elizabeth M
authors.initials: EM
authors.lastname: Collantes
authors.forename: Seung Won
authors.initials: SW
authors.lastname: Chung
authors.forename: Charlene
authors.initials: C
authors.lastname: Desbonnet
authors.forename: Jonathan
authors.initials: J
authors.lastname: Doty
authors.forename: Matthew
authors.initials: M
authors.lastname: Doroski
authors.forename: Juntyma J
authors.initials: JJ
authors.lastname: Engtrakul
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Harris
authors.forename: Michael
authors.initials: M
authors.lastname: Huband
authors.forename: John D
authors.initials: JD
authors.lastname: Knafels
authors.forename: Karen L
authors.initials: KL
authors.lastname: Leach
authors.forename: Shenping
authors.initials: S
authors.lastname: Liu
authors.forename: Anthony
authors.initials: A
authors.lastname: Marfat
authors.forename: Andrea
authors.initials: A
authors.lastname: Marra
authors.forename: Eric
authors.initials: E
authors.lastname: McElroy
authors.forename: Michael
authors.initials: M
authors.lastname: Melnick
authors.forename: Carol A
authors.initials: CA
authors.lastname: Menard
authors.forename: Justin I
authors.initials: JI
authors.lastname: Montgomery
authors.forename: Lisa
authors.initials: L
authors.lastname: Mullins
authors.forename: Mark C
authors.initials: MC
authors.lastname: Noe
authors.forename: John
authors.initials: J
authors.lastname: O'Donnell
authors.forename: Joseph
authors.initials: J
authors.lastname: Penzien
authors.forename: Mark S
authors.initials: MS
authors.lastname: Plummer
authors.forename: Loren M
authors.initials: LM
authors.lastname: Price
authors.forename: Veerabahu
authors.initials: V
authors.lastname: Shanmugasundaram
authors.forename: Christy
authors.initials: C
authors.lastname: Thoma
authors.forename: Daniel P
authors.initials: DP
authors.lastname: Uccello
authors.forename: Joseph S
authors.initials: JS
authors.lastname: Warmus
authors.forename: Donn G
authors.initials: DG
authors.lastname: Wishka
mesh_terms: D000581:Amidohydrolases / Q000037:antagonists & inhibitors*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020134:Catalytic Domain; D018360:Crystallography, X-Ray; D024881:Drug Resistance, Bacterial; D006860:Hydrogen Bonding; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D010647:Phenyl Ethers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011552:Pseudomonas Infections / Q000188:drug therapy*; D011550:Pseudomonas aeruginosa; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013450:Sulfones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D001713:Biphenyl Compounds; D006877:Hydroxamic Acids; D010647:Phenyl Ethers; D013440:Sulfides; D013450:Sulfones; D000581:Amidohydrolases; C514484:LpxC deacetylase, Pseudomonas; C097307:UDP-3-O-acyl-N-acetylglucosamine deacetylase