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新型抗疟药2-[3-(7-氯喹啉-4-基氨基)-烷基]-1-(取代苯基)-2,3,4,9-四氢-1H-β-咔啉的合成

Synthesis of 2-[3-(7-Chloro-quinolin-4-ylamino)-alkyl]-1-(substituted phenyl)-2,3,4,9-tetrahydro-1H-beta-carbolines as a new class of antimalarial agents.

作者信息

Gupta Leena, Srivastava Kumkum, Singh Shubhra, Puri S K, Chauhan Prem M S

机构信息

Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.

出版信息

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3306-9. doi: 10.1016/j.bmcl.2008.04.030. Epub 2008 Apr 15.

DOI:10.1016/j.bmcl.2008.04.030
PMID:18442907
Abstract

A series of hybrid molecules 2-[3-(7-Chloro-quinolin-4-ylamino)-alkyl]-1-(substituted phenyl)-2,3,4,9-tetrahydro-1H-beta-carbolines have been synthesized and screened for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum. Compounds 26, 32, and 34 have shown MIC in the range of 0.05-0.11 microM and are in vitro several folds more active than chloroquine.

摘要

已经合成了一系列杂化分子2-[3-(7-氯喹啉-4-基氨基)-烷基]-1-(取代苯基)-2,3,4,9-四氢-1H-β-咔啉，并对其针对恶性疟原虫氯喹敏感株的体外抗疟活性进行了筛选。化合物26、32和34的最低抑菌浓度在0.05-0.11微摩尔范围内，并且在体外比氯喹活性高几倍。

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