Author/Authors :
Judy Hayler، نويسنده , , Peter D. Kane، نويسنده , , Darren LeGrand، نويسنده , , Florence Lugrin، نويسنده , , Keith Menear، نويسنده , , Richard Price، نويسنده , , Mark Allen، نويسنده , , Xiaoling Cockcroft، نويسنده , , John Ambler، نويسنده , , Keith Butler، نويسنده , , Karren Dunnet، نويسنده , , Andrew Mitchelson، نويسنده , , Mark Talbot، نويسنده , , Morris Tweed، نويسنده , , Nicholas Wills، نويسنده ,
Abstract :
The further optimisation of the novel lead compound CGH752 (Fig. 1) is described. By introducing various substituents into the 6-position of the 3,3-dimethyltetrahydroquinoline (DMTHQS) ring we have been able to favourably affect the in vitro and in vivo activity, and the pharmacokinetics of such compounds. One of the inhibitors synthesised (CGH1484) is bioavailable and shows efficacy in animal models of thrombosis.
