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Design and Synthesis of New N-OMe Fluoro-Indole Melatoninergics

[ Vol. 3 , Issue. 6 ]

Author(s):

A. Tsotinis, J. Gourgourinis, A. Eleutheriades, K. Davidson and D. Sugden   Pages 561 - 571 ( 11 )

Abstract:


The synthesis of a series of new N-OMe fluoro-indoles with melatoninergic activity in the Xenopus melanophore assay is described. All of the 4-F substituted compounds, 22a-e and 25a,b, were antagonists on the clonal Xenopus melanophore line. Conversely, the 5-F substituted analogs (15a-e) did not share the same pharmacological profile, as two of them, compounds 15d (R=c-C3H5) and 15e (R=c-C4H7), exhibited a weak agonistic and partial agonistic activity, respectively, whilst the other three (15a-c) were all agonists. It seems that in this case the nature of the response (agonist or antagonist activity) is solely dependent on the shape of the R group.

Keywords:

N-OMe fluoro-indoles, synthesis, melatoninergic potency, structure activity relationships

Affiliation:

Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli- Zografou, 157 71 Athens, Greece.



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