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Figure 3. Bound conformation of 1 (magenta) and 7a (green) in the
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of in vitro active series. Further optimization will be
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Acknowledgments
The authors extend their gratitude to Dr. Frank H. Ebe-
tino and Dr. John A. Wos for the invaluable technical
discussions and assistance.
14. Gupta, R. R.; Kumar, M.; Gupta, V. Heterocyclic
Chemistry I; Spinger-Verlag: Germany, 1998.
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Appl., 78703, 11 May 1983; (b) 7a–r: a mixture of the
corresponding nitro-guanidine compound (0.25 mmol) and
5% Pd/BaSO4 (15 mg) in 20% AcOH/MeOH (3 mL) was
stirred for 8–12 h under H2 atmosphere. The mixture
diluted with MeOH (5 mL) and filtered through a syringe-
filter (0.45 lm). The filtrates purified by preparative HPLC
(Polaris C18-A 10l, 250 · 500 R, 1% TFA-water/acetoni-
trile as eluent) to yield the desired products as TFA
salts.
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16. MCH functional antagonist was detected using HEK 293
cells that expressed the MCH-R1 (SLC-1) receptor in a
firefly luciferase reporter assay. Cells were incubated for
4 h in the presence of 25 nM MCH and varying concen-
trations of drug of interest. Receptor activation was
measured by luminescence.