Synthesis and morphine enhancement activity of N-[5-(2-phenoxyphenyl)-1 3,4-oxadiazole-2-yl]-N′-phenylurea derivatives

被引:3
|
作者
Rad, AA
Sheikhha, M
Hosseini, R
Tabatabai, SA
Shafiee, A
机构
[1] Univ Tehran Med Sci, Dept Med Chem, Fac Pharm, Tehran, Iran
[2] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Fac Pharm, Tehran, Iran
[3] Univ Tehran Med Sci, Dept Pharmacol & Toxicol, Fac Pharm, Tehran, Iran
[4] Shaheed Beheshti Univ Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran
关键词
1,3,4-oxadiazole; L-365,260, CCK-B antagonist; morphine enhancement; analgesia;
D O I
10.1002/ardp.200300822
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of N-[5-(2-phenoxyphenyl)-1,3,4-oxadiazole-2-yl]-N'-phenylurea derivatives is reported. The structures of these compounds are supported by their IR, (1)H-NMR and mass spectra. Conformational analysis and superimposition of energy minima conformers of these compounds on L-365,260, a known 3-ureido-1 4-benzodiazepine CCK-B antagonist, showed that the aromatic rings fell in the same contour. Morphine analgesia enhancement evaluation of the synthesized compounds in comparison with a control group showed that compounds 8a, 8c, 8h-8j, 8l, 8o have significant effects.
引用
收藏
页码:193 / 200
页数:8
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