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Synthesis of new tricyclic melatoninergic ligands
A Tsotinis1, M Panoussopoulou, S Sivananthan
1School of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Greece. tsotinis@pharm.uoa.gr
Abstract:
We report the synthesis and biological evaluation of a series of new tricyclic analogs of the hormone melatonin, which act as probes of the constraints at the hormone's receptor site with regard to the lower N1-C2 region of the indole moiety of melatonin. Three of the new compounds, N-[2-(2-methoxy-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl)ethyl]acetamide (9), and the respective propionamide 10 and butyramide 11, are as potent as melatonin in the Xenopus laevis melanophore model.