Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase

  • Bioorg Med Chem Lett. 2002 Oct 21;12(20):2931-4. doi: 10.1016/s0960-894x(02)00600-5.
Edwin J Iwanowicz  1 ,  Scott H Watterson ,  Chunjian Liu ,  Henry H Gu ,  Toomas Mitt ,  Katerina Leftheris ,  Joel C Barrish ,  Catherine A Fleener ,  Katherine Rouleau ,  N Z Sherbina ,  Diane L Hollenbaugh
Affiliations
  • 1. Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. [email protected]
Abstract

A series of novel guanidine-based small molecule inhibitors of Inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in Guanine Nucleotide biosynthesis and is a target for Anticancer, immunosuppressive and Antiviral therapy. The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.