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and suspended in a 1:1:4:4 mixture of glycerol, water, gelatin, and
CMC. Administered doses were from 0.3 to 100 mg/kg rat (1m:
3-100 mg/kg) (n ) 4/group). Before dosing and up to 8 h post
dose, a blood sample was collected by puncture of the tail vein.
Plasma insulin was measured with a rat-specific ELISA, and the
results were reported as percent decrease in insulin levels from the
rat’s own baseline. The maximal efficacy was, in pilot experiments,
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value for the compounds tested (Table 2).
Acknowledgment. We thank Anette Koch and Jørn Ole
Lund for technical assistance with the syntheses and Flemming
Gundertofte for the elemental analyses. We thank Dr. Petra
Wiede for growing the single crystals and solving crystal
structures of compound 2.
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Supporting Information Available: Screening experiments for
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1a; details of crystal structure data and refinement of 1a, polymorph
A; details of crystal structure data and refinement of 2; elemental
analyses of compounds 1c-p, 5, 14, and 18a,b. This material is
609647 contains the supplementary crystallographic data for
compound 1a. The data can be obtained free of charge from The
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