Abstract:
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.