title: Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.
abstract: The synthesis and the structure-activity relationships (SAR) of analogues derived from the introduction of basic residues on ring D of quinolone-based inhibitors of IMPDH are described. This led to the identification of compound 27 as a potent inhibitor of IMPDH with significantly improved aqueous solubility over the lead compound 1.
authors.affiliation: Bristol-Myers Squibb PRI, Princeton, NJ 08543-4000, USA. dharm@bms.com
authors.forename: T G Murali
authors.initials: TG
authors.lastname: Dhar
authors.forename: Scott H
authors.initials: SH
authors.lastname: Watterson
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Zhongqi
authors.initials: Z
authors.lastname: Shen
authors.forename: Henry H
authors.initials: HH
authors.lastname: Gu
authors.forename: Derek
authors.initials: D
authors.lastname: Norris
authors.forename: Marianne
authors.initials: M
authors.lastname: Carlsen
authors.forename: Kristin D
authors.initials: KD
authors.lastname: Haslow
authors.forename: William J
authors.initials: WJ
authors.lastname: Pitts
authors.forename: Junqing
authors.initials: J
authors.lastname: Guo
authors.forename: John
authors.initials: J
authors.lastname: Chorba
authors.forename: Catherine A
authors.initials: CA
authors.lastname: Fleener
authors.forename: Katherine A
authors.initials: KA
authors.lastname: Rouleau
authors.forename: Robert
authors.initials: R
authors.lastname: Townsend
authors.forename: Diane
authors.initials: D
authors.lastname: Hollenbaugh
authors.forename: Edwin J
authors.initials: EJ
authors.lastname: Iwanowicz
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D015363:Quinolones; D007168:IMP Dehydrogenase