Synthesis of Bergenin Derivatives, Biocatalytic Reactions, Microorganisms, Nuclear Magnetic Resonance, Spectroscopy

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Synthesis of Bergenin Derivatives

Bergenin is a flavonoid and has been used as a lead compound for getting a library of derivatives that can be screened for drug discovery. In this study, a broad range of biocatalytic reactions have been used, in two rounds, for an automated, iterative synthesis of a 600-member library For this purpose, 16 purified enzymes and 25 microorganisms that were capable of accepting bergenin as a substrate were initially selected and used. Successful generation of each derivative was confirmed by high throughput mass spectrometry and by nuclear magnetic resonance (NMR) spectroscopy. The library was then screened for targets such as xanthine oxidase (for treatment of gout and multiple sclerosis) and urokinase (an anticancer target). Inhibitors, much better than bergenin were detected and resynthesis and confirmation of derivatives may give one or more drugs.

Synthesis of Bergenin Derivatives

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