Synthesis and biological evaluation of flavonoids and related compounds as gastroprotective agents
โ Scribed by Jeffrey J. Ares; Pamela E. Outt; Jared L. Randall; Jeffrey N. Johnston; Peter D. Murray; Linda M. O'Brien; Pamela S. Weisshaar; Beth L. Ems
- Publisher
- Elsevier Science
- Year
- 1996
- Tongue
- English
- Weight
- 208 KB
- Volume
- 6
- Category
- Article
- ISSN
- 0960-894X
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โฆ Synopsis
Several analogs of the gastroprotective molecule flavone have been synthesized and evaluated for gastroprotective activity. A C2-C3 double bond and an intact C ring appear necessary for optimum activity. Activity can be retained by replacing the 2-phenyl substituent with other groups but is eliminated when this ring is moved from the 2-to the 3-position.
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An efficient and novel process is described for the synthesis of nectrisine 5 and its related derivatives 6,'/as potent glucosidase inhibitors via the corresponding lactams starting from D-(-)-diethyl tara'ate. Also the results of biological evaluation of the synthesized compounds are described.