Pyrimidine benzamide-based thrombopoietin receptor agonists

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5447-54. doi: 10.1016/j.bmcl.2007.07.038. Epub 2007 Jul 31.

Abstract

A series of pyrimidine benzamide-based thrombopoietin receptor agonists is described. The lead molecule contains a 2-amino-5-unsubstituted thiazole, a group that has been associated with idiosyncratic toxicity. The potential for metabolic oxidation at C-5 of the thiazole, the likely source of toxic metabolites, was removed by substitution at C-5 or by replacing the thiazole with a thiadiazole. Potency in the series was improved by modifying the substituents on the pyrimidine and/or on the thiazole or thiadiazole pendant aryl ring. In vivo examination revealed that compounds from the series are not highly bioavailable. This is attributed to low solubility and poor permeability.

MeSH terms

  • Antigens, CD34 / metabolism
  • Benzamides / chemical synthesis*
  • Benzamides / pharmacokinetics
  • Benzamides / pharmacology*
  • Cell Differentiation / drug effects
  • Cell Line
  • Cell Proliferation / drug effects
  • Chemical Phenomena
  • Chemistry, Physical
  • Computer Simulation
  • Cross Reactions
  • Drug Evaluation, Preclinical
  • Humans
  • Molecular Weight
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacokinetics
  • Pyrimidines / pharmacology*
  • Receptors, Thrombopoietin / agonists*
  • Solubility
  • Structure-Activity Relationship

Substances

  • Antigens, CD34
  • Benzamides
  • Pyrimidines
  • Receptors, Thrombopoietin