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
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.