Himbacine derived thrombin receptor (PAR-1) antagonists: structure-activity relationship of the lactone ring |
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| Authors: | Xia Yan Chackalamannil Samuel Chan Tze-Ming Czarniecki Michael Doller Darío Eagen Keith Greenlee William J Tsai Hsingan Wang Yuguang Ahn Ho-Sam Boykow George C McPhail Andrew T |
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| Affiliation: | Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. yan.xia@spcorp.com |
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| Abstract: | The structure-activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagonists (e.g., 2-5) is described. The effect of the lactone carbonyl group on binding to PAR-1 is dependent on the substitution pattern of the pyridine ring. A stereoselective intramolecular Michael addition reaction to the vinyl pyridine group was observed for these pyridine analogs of himbacine in basic conditions at elevated temperature. |
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