环取代4-氨基喹啉的合成及其抗疟活性评价。
Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities.
作者信息
Madrid Peter B, Sherrill John, Liou Ally P, Weisman Jennifer L, Derisi Joseph L, Guy R Kiplin
机构信息
Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94143-2280, USA.
出版信息
Bioorg Med Chem Lett. 2005 Feb 15;15(4):1015-8. doi: 10.1016/j.bmcl.2004.12.037.
A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.
采用一种简单的两步合成方法制备了51种B环取代的4-羟基喹啉，以便分析环取代对恶性疟原虫（疟疾发病的主要原因）氯喹敏感株和耐药株生长抑制的影响。发现除氯喹中的7-氯喹啉环外的取代喹啉环对恶性疟原虫W2耐药株具有显著活性。
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