Literature DB >> 12668009

High-throughput synthesis and optimization of thrombin inhibitors via urazole alpha-addition and Michael addition.

P Douglas Boatman1, Jan Urban, Minh Nguyen, Maher Qabar, Michael Kahn.   

Abstract

A novel alpha-addition of propiolates to urazoles followed by Michael addition of a variety of nucleophiles has been developed for rapid production and optimization of peptidomimetic drug leads. This technology has produced a number of highly potent and selective inhibitors of the serine protease, thrombin.

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Year:  2003        PMID: 12668009     DOI: 10.1016/s0960-894x(03)00155-0

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


  1 in total

1.  One-pot and efficient synthesis of triazolo[1,2-a]indazole-triones via reaction of arylaldehydes with urazole and dimedone catalyzed by silica nanoparticles prepared from rice husk.

Authors:  Hooshang Hamidian; Samieh Fozooni; Asadollah Hassankhani; Sayed Zia Mohammadi
Journal:  Molecules       Date:  2011-10-26       Impact factor: 4.411

  1 in total

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