Fluorination of 3-(3-(piperidin-1-yl) propyl) indoles and 3-(3-(piperazin-1-yl) propyl) indoles gives selective human 5-HT1D receptor ligands with improved …

…, KL Locker, AM MacLeod, D Morrison…

Index: Van Niel, Monique B.; Collins, Ian; Beer, Margaret S.; Broughton, Howard B.; Cheng, Susan K. F.; Goodacre, Simon C.; Heald, Anne; Locker, Karen L.; MacLeod, Angus M.; Morrison, Denise; Moyes, Christopher R.; O'Connor, Desmond; Pike, Andrew; Rowley, Michael; Russell, Michael G. N.; Sohal, Baibinder; Stanton, Josephine A.; Thomas, Steven; Verrier, Hugh; Watt, Alan P.; Castro, Jose L. Journal of Medicinal Chemistry, 1999 , vol. 42, # 12 p. 2087 - 2104

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Citation Number: 101

Abstract

It has previously been reported that a 3-(3-(piperazin-1-yl) propyl) indole series of 5-HT1D receptor ligands have pharmacokinetic advantages over the corresponding 3-(3-(piperidin-1- yl) propyl) indole series and that the reduced p K a of the piperazines compared to the piperidines may be one possible explanation for these differences. To investigate this proposal we have developed versatile synthetic strategies for the incorporation of fluorine ...