Alizadeh Babak Heidary, Foroumadi Alireza, Ardestani Susan K, Poorrajab Fatemeh, Shafiee Abass
Iranian Research Institute of Plant Protection, Tehran, Iran.
Arch Pharm (Weinheim). 2008 Dec;341(12):787-93. doi: 10.1002/ardp.200800128.
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%.
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%。