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

✍ Scribed by Patrick Roussel; Mark Bradley; Peter Kane; Christine Bailey; Ruth Arnold; Andrew Cross

Book ID
104209378
Publisher
Elsevier Science
Year
1999
Tongue
French
Weight
754 KB
Volume
55
Category
Article
ISSN
0040-4020

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✦ Synopsis

Following a high throughput screen (HTS) for the inhibition of the tissue factor/factor Vlla 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 had an ICso of 411M some 10x more potent than the original lead compound.

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