Bioorganic and Medicinal Chemistry p. 2767 - 2773 (1999)
Update date:2022-08-03
Topics:
Bromidge, Steven M.
Dabbs, Steven
Davies, David T.
Davies, Susannah
Duckworth, D.Malcolm
Forbes, Ian T.
Gadre, Angela
Ham, Peter
Jones, Graham E.
King, Frank D.
Saunders, Damian V.
Thewlis, Kevin M.
Vyas, Deepa
Blackburn, Thomas P.
Holland, Vicky
Kennett, Guy A.
Riley, Graham J.
Wood, Martyn D.
A model series of 5-HT(2C) antagonists have been prepared by rapid parallel synthesis. These N-substituted phenyl-N'-pyridin-3-yl ureas were found to have a range of 5-HT(2C) receptor affinities and selectivities over the closely related 5-HT(2A) receptor. Extrapolation of simple SAR, derived from this set of compounds, to the more active but synthetically more complex 1-(3-pyridyl-carbamoyl)indoline series allowed us to target optimal substitution patterns and identify potent and selective 5-HT(2C/2B) antagonists. Copyright (C) 1999 Elsevier Science Ltd.
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