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Increase by Optimization of Aromatic Substituents. -Starting from a screening hit a novel series of compounds such as (IV) is synthesized. Derivative (IVc) is about 100000-fold more active as DPP-IV inhibitor compared to the original found substance. An X-ray analysis reveals that compound (IVc) binds to the active site of the enzyme. -(PETERS*, J.-U.; WEBER, S.; KRITTER, S.; WEISS, P.; WALLIER, A.; BOEHRINGER, M.; HENNIG, M.; KUHN, B.; LOEFFLER, B.-M.; Bioorg. Med.

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