A series of substituted pyrrolidine-2,4-dicarboxylic acid amides were synthesized as potential antidiabetic agents, and many of them showed good in vitro DPP-IV inhibition (IC50 = 2-250 nM) with selectivity over DPP-II, DPP8, and FAP enzymes. Selected compounds 8c and 11a showed in vivo plasma DPP-IV inhibition after oral administration in Wistar rats.
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Chlorine-substituted transformation products generated during chlorination of the organophosphorus insecticide disulfoton induce anti-acetylcholine esterase activity.
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Faculty of Engineering, Hokkaido University, N13W8, Sapporo, 060-8628, Japan. Electronic address:
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