Proceedings of the PSK Conference (대한약학회:학술대회논문집)
- 2002.10a
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- Pages.347.4-348
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- 2002
Synthesis and Antiinflammatory Activity of 1.5- and 4.5-Disubstituted Imidazoles
- Tuyen, Truong-Ngoc (College of Pharmacy kangwon National University) ;
- Sin, Kwan-Seog (College of Pharmacy kangwon National University) ;
- Kim, Hyun-Pyo (College of Pharmacy kangwon National University) ;
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Park, Hae-Il
(College of Pharmacy kangwon National University)
- Published : 2002.10.01
Abstract
Recently it has been demonstrated that selective cyclooxygenase-2 (COX-2) inhibitors retain the antiinflammatory effect but with markedly reduced GI toxicity compared to non selective inhibitors such as traditional NSAIDs. As a consequence, intense efforts have been made to develop selective COX-2 inhibtors during the last decade. Two compounds in this class. celecoxib and rofecoxib. are already in the market and are proved as potent and selective COX-2 inhibitors with much better gastric tolerance. However. there are still strong domands for a COX-2 inhibitor with improved efficacy and safety profiles. Here we report the synthesis and biological profiles of 1.5- and 4.5-disubstituted imidazole analogues as structural equivalents of cefecoxib and refecoxib. The imidazole analogues are overlapped well whth the 3D srructures of celecoxib and rofecoxib.
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