Literature DB >> 12113805

Combinatorial synthesis and biological evaluation of isoxazole-based libraries as antithrombotic agents.

S Batra1, T Srinivasan, S K Rastogi, B Kundu, A Patra, A P Bhaduri, M Dixit.   

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.

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Year:  2002        PMID: 12113805     DOI: 10.1016/s0960-894x(02)00333-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Solution phase synthesis of a diverse library of highly substituted isoxazoles.

Authors:  Jesse P Waldo; Saurabh Mehta; Benjamin Neuenswander; Gerald H Lushington; Richard C Larock
Journal:  J Comb Chem       Date:  2008-08-01

2.  A surprising new route to 4-nitro-3-phenylisoxazole.

Authors:  Henning Hopf; Aboul-Fetouh E Mourad; Peter G Jones
Journal:  Beilstein J Org Chem       Date:  2010-06-23       Impact factor: 2.883

3.  Isoxazole derivatives as new nitric oxide elicitors in plants.

Authors:  Anca Oancea; Emilian Georgescu; Florentina Georgescu; Alina Nicolescu; Elena Iulia Oprita; Catalina Tudora; Lucian Vladulescu; Marius-Constantin Vladulescu; Florin Oancea; Calin Deleanu
Journal:  Beilstein J Org Chem       Date:  2017-04-06       Impact factor: 2.883

  3 in total

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