A facile regioselective synthesis of novel spiro-thioxanthene and spiro-xanthene-9′,2-[1,3,4]thiadiazole derivatives as potential analgesic and anti-inflammatory agents

被引：244

作者：

Hafez, H. N. ^{[1
]}

Hegab, M. I. ^{[1
]}

Ahmed-Farag, I. S. ^{[2
]}

El-Gazzar, A. B. A. ^{[1
]}

机构：

[1] Natl Res Ctr, Photochem Dept, Giza 12622, Egypt

[2] Natl Res Ctr, Dept Solid State Phys, Xray Lab, Giza 12622, Egypt

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 16期

关键词：

spiro-thioxanthene; spiro-xanthene-9 ',2-[1,3.4]thiadiazole; single crystal X-ray structural analysis; anti-inflammatory and analgesic activities;

D O I：

10.1016/j.bmcl.2008.07.042

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

The 1,3-dipolar cycloaddition of nitrile immes to 9H-thioxanthone-9-thione and 9H-xanthone-9-thione afforded novel spiro-thioxanthene-9',2-[1,3,4] thiadiazoles 6a-g and spiro-xanthene-9',2-[1,3,4]thiadiazoles 7a-g in good yields. Some of the newly synthesized compounds were tested for anti-inflammatory and analgesic activities comparable to ibuprofen. Compounds 6a,d,e and 7a,d,e showed significant activity compared to standard drug. The toxicity studies revealed that neither death nor other behavioral or toxicological changes were observed on rats up to a dose as high as 200 mg/kg. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4538 / 4543

页数：6

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