【摘要】 <正> 2,4-二氨基-6-取代苄氨基喹唑啉类化合物有较强的抗疟作用,其中2,4-二氨基-6-[(3,4-二氯苄基)-N-亚硝基-氨基]喹唑啉(Ⅰ,硝喹)经国内研究已用于临床,对抗氯喹恶性疟也有较好的作用。为了进一步探讨其构效关系,作者合成了一系列2,4-二氨基2-氨基-4-羟基和2,4-二羟基-6-取代氨基喹唑啉类化合物。更多还原

【Abstract】 2,4-Diamino-, 2-amino-4-hydroxy-and 2,4-dihydroxy-6-substituted amino quinazolines were synthesized and evaluated for their antimalarial activities. Preliminary screening tests conducted on mice infected with Plasmodium berghei showed that most compounds of Ⅱ and Ⅲ were effective in varying degrees in the blood schizonticidal test, with compounds Ⅲ_2～4 being as effective as nitroquine. Compounds V were found to have some effects, but compounds of Ⅳ, Ⅵ and Ⅶ were shown to be inactive.更多还原