SYNTHESIS OF NEW PYRROLO[1,2-D][1,2,4]TRIAZINES AND THIAZOLO[3,4-D][1,2,4]TRIAZINES AS IMMUNOSTIMULATING AGENTS

Four pyrrolo[1,2-d][1,2,4]triazines and four thiazolo[3,4-d][1,2,4]tri azines were synthesized from trans-4-hydroxy-L-proline and L-thiaproli ne, respectively. The synthetic route involved formation of hydrazides followed by cyclization with orthoesters. The proliferative response to human lymphocyte mitogen (phytohemagglutinin) revealed significant immunostimulant activity for all test drugs. Furthermore, some triazin e derivatives were effective to activate production of free oxygen rad ical by phagocytes in response to stimulation by opsonized zymosan. (C ) 1998 Elsevier Science Ltd. All rights reserved.