Triazinediones as prokineticin 1 receptor antagonists. Part 1: SAR, synthesis and biological evaluation.

A series of guanidine triazinediones were identified as potent PK1 receptor antagonists. A compound in this series inhibited the PK1 invoked prosecretory response in rat ileum tissue.

Improved solution- and solid-phase preparation of hydroxamic acids from esters.

The addition of small amounts of solid KCN to solution and solid-phase esters in THF/MeOH/50% aqueous NH2OH increases the efficiency of their transformation to the corresponding hydroxamic acids.