2. Academic Validation
  3. Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues

Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues

  • Bioorg Med Chem Lett. 2003 Feb 10;13(3):547-51. doi: 10.1016/s0960-894x(02)00945-9.
T G Murali Dhar 1,  Scott H Watterson,  Ping Chen,  Zhongqi Shen,  Henry H Gu,  Derek Norris,  Marianne Carlsen,  Kristin D Haslow,  William J Pitts,  Junqing Guo,  John Chorba,  Catherine A Fleener,  Katherine A Rouleau,  Robert Townsend,  Diane Hollenbaugh,  Edwin J Iwanowicz
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb PRI, Princeton, NJ 08543-4000, USA. dharm@bms.com
PMID: 12565969 DOI: 10.1016/s0960-894x(02)00945-9
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.

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