STUDIES ON NEW ANTIMALARIALS——SYNTHESIS OF HETEROCYCLIC COMPOUNDS CARRYING DOUBLE MANNICH BASIC CHAINS OF p-AMINOPHENOL

This paper presents the preparation of heterocyclic compounds V_1～19 carrying double Mannich basic side chains of p-aminophenol. These heterocyclic nuclei are benzo g quinoline, 1,5-naphthyridine, pyrido2,3-dpyrimidine, benzocacridine, pyrido2,3-c acridine and pyrido2,3-eacridine. Compounds V_1～19 were synthesized from the heterocyclic intermediates a～f by condensing with p-aminophenol. Products Ⅵ carrying p-aminophenoi reacted further with Mannich reagents to yield the desired compounds.Compounds V_{1～3, 6, 8～15, 19} were tested for blood schizonticidal activity against Plasmodium berghei in mice. The results showed that compounds V_{1～3, 8, 10, 12, 19} were rather effective. In addition, compounds V_{4～10, 16, 19} did not show any activity in P. yoelii-Anopheles stephensi-mouse model.