Author/Authors :
Yan Xia، نويسنده , , Samuel Chackalamannil، نويسنده , , Tze-Ming Chan، نويسنده , , Michael Czarniecki، نويسنده , , Dario Doller، نويسنده , , Keith Eagen، نويسنده , , William J. Greenlee، نويسنده , , Hsingan Tsai، نويسنده , , Yuguang Wang، نويسنده , , Ho-Sam Ahn، نويسنده , , George C. Boykow، نويسنده , , Andrew T. McPhail، نويسنده ,
Abstract :
The structure–activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagoinsts (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.
Keywords :
structure–activity relationship , Himbacine , Thrombin receptor antagonist , PAR-1 Antagonist
