SYNTHESIS AND POTENTIAL ANTIALLERGIC ACTIVITY OF NEW PTERIDINONES ANDRELATED-COMPOUNDS

The synthesis and pharmacological profile of a series of 2-alkoxy and 2-phenoxymethyl-3H-pteridin-4-ones and related compounds are described . These compounds displayed antiallergic activity in the passive cutan eous anaphylaxis test in rats. In contrast to both sodium cromoglycate and nedocromil sodium, many of our compounds were active when adminis tered orally. The most potent in this series, 2-ethoxymethyl-3H-pterid in-4-one 2b (LCB 2183) was investigated in other models of allergy and inflammation. The antiallergic activity was confirmed and interesting antiinflammatory properties were observed. It was therefore selected for further development as a human therapeutic agent.