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新型取代喹唑啉衍生物作为抗利什曼原虫剂的设计与合成

Design and synthesis of novel substituted quinazoline derivatives as antileishmanial agents.

作者信息

Agarwal K C, Sharma Vidisha, Shakya Nishi, Gupta Suman

机构信息

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

出版信息

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5474-7. doi: 10.1016/j.bmcl.2009.07.081. Epub 2009 Jul 19.

Abstract

4-(Substituted-benzylidine)-2-substituted-5,6-dihydrobenzo[h]quinazoline (5a-p) and 4-(substituted-benzylidine)-2-substituted-3, 4, 5, 6-tetrahydrobenzo[h]quinazoline (6a-p) have been synthesized from 2-(substituted-benzylidine)tetralone-1(3a-d) and several substituted guanidine sulfates(4a-d).These compounds were tested for their in vitro antileishmanial activity. The compounds 6i, 6f, 6g show promising antileishmanial activity against Leishmania donovani.

摘要

4-(取代亚苄基)-2-取代-5,6-二氢苯并[h]喹唑啉(5a-p)和4-(取代亚苄基)-2-取代-3,4,5,6-四氢苯并[h]喹唑啉(6a-p)由2-(取代亚苄基)-1,2,3,4-四氢萘酮-1(3a-d)和几种取代胍硫酸盐(4a-d)合成。对这些化合物进行了体外抗利什曼原虫活性测试。化合物6i、6f、6g对杜氏利什曼原虫显示出有前景的抗利什曼原虫活性。

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