Inhibition of the tissue factor/factor VIIa complex—Lead optimisation using combinatorial chemistry

P Roussel, M Bradley, P Kane, C Bailey, R Arnold…

Index: Roussel, Patrick; Bradley, Mark; Kane, Peter; Bailey, Christine; Arnold, Ruth; Cross, Andrew Tetrahedron, 1999 , vol. 55, # 19 p. 6219 - 6230

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Citation Number: 42

Abstract

Following a high throughput screen (HTS) for the inhibition of the tissue factor/factor VIIa complex and the identification of a number of original hits a lead optimisation programme was initiated to improve their potency. This necessitated the development of an amidine based linker which allowed the generation of a library of amidinonaphthols prepared both by multiple parallel synthesis (MPS) and split and mix methods. The most active compound ...