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Combinatorial synthesis and biological evaluation of isoxazole-based libraries as antithrombotic agents
S Batra1, T Srinivasan, S K Rastogi
1Medicinal Chemistry Division, Central Drug Research Institute, Lucknow 226001, India. batra_san@yahoo.co.uk
Bioorganic & Medicinal Chemistry Letters
|July 13, 2002
Abstract:
The 3-substituted phenyl-5-isoxazolecarboxaldehydes have been identified as activated aldehydes for the generation of isoxazole-based combinatorial libraries on solid phase through automation. Three highly functionalized isoxazole-based libraries comprising of 32, 96 and 45 compounds each have been synthesized in parallel format using Baylis Hillman reaction, Michael addition, reductive amination and alkylation reactions. With an objective of lead generation all the three libraries were evaluated for their antithrombin activity in vivo.