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新型合成色烯的杀利什曼原虫评估

Leishmanicidal evaluation of novel synthetic chromenes.

作者信息

Alizadeh Babak Heidary, Foroumadi Alireza, Ardestani Susan K, Poorrajab Fatemeh, Shafiee Abass

机构信息

Iranian Research Institute of Plant Protection, Tehran, Iran.

出版信息

Arch Pharm (Weinheim). 2008 Dec;341(12):787-93. doi: 10.1002/ardp.200800128.

Abstract

In the present paper, twelve chromenes were synthesized by coupling of 2,2,8,8-tetramethyl-8H-pyrano[2,3-f]chroman-4-one 1 with various aryl and benzylmagnesium chlorides. The synthetic compounds were examined for in-vitro activity against Leishmania major, and some of them displayed efficient anti-leishmanial activity. Among the compounds tested, compounds 9 (4-(2-chloro-benzylidene)-2,2,8,8-tetramethyl-3,4-dihydro-2H,8H-pyrano[2,3-f]chromene 9a and 4-(2-chloro-benzyl)-2,2,8,8-tetramethyl-2H,8H-pyrano[2,3-f]chromene 9b) were the most active with an inhibitory activity of 73.4%.

摘要

在本论文中,通过2,2,8,8-四甲基-8H-吡喃并[2,3-f]色满-4-酮1与各种芳基和苄基氯化镁偶联合成了12种色烯。对合成的化合物进行了抗杜氏利什曼原虫的体外活性检测,其中一些表现出有效的抗利什曼活性。在所测试的化合物中,化合物9(4-(2-氯亚苄基)-2,2,8,8-四甲基-3,4-二氢-2H,8H-吡喃并[2,3-f]色烯9a和4-(2-氯苄基)-2,2,8,8-四甲基-2H,8H-吡喃并[2,3-f]色烯9b)活性最高,抑制活性为73.4%。

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