184041-52-9Relevant academic research and scientific papers
The design and synthesis of thrombin inhibitors: The introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors
Hayler, Judy,Kane, Peter D.,Legrand, Darren,Lugrin, Florence,Menear, Keith,Price, Richard,Allen, Mark,Cockcroft, Xiaoling,Ambler, John,Butler, Keith,Dunnet, Karren,Mitchelson, Andrew,Talbot, Mark,Tweed, Morris,Wills, Nicholas
, p. 1567 - 1570 (2000)
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. (C) 2000 Elsevier Science Ltd. All rights reserved.
