Abstract
The imidazole-4,5-dicarboxylic acid scaffold is readily derivatized with amino acid esters to afford symmetrically- and dissymmetrically-disubstituted imidazole-4,5-dicarboxamides with intramolecularly hydrogen bonded conformations that predispose the presentation of amino acid pharmacophores. In this work, a total of 45 imidazole-4,5-dicarboxamides bearing amino acid esters were prepared by parallel synthesis. The library members were purified by column chromatography on silica gel and the purified compounds characterized by LC-MS with LC detection at 214 nm. A selection of the final compounds was also analyzed by 1H-NMR spectroscopy. The analytically pure final products have been submitted to the Molecular Library Small Molecule Repository (MLSMR) for screening in the Molecular Library Screening Center Network (MLSCN) as part of the NIH Roadmap.
Highlights
Small molecule biological probes that influence protein function are useful tools for studying the cell and can serve as lead structures in the development of new therapeutic agents [1,2,3,4,5]
This paper describes the synthesis and characterization of an imidazole-4,5-dicarboxamide (I45DC)
We have been using the imidazole-4,5-dicarboxylic acid (I45DA) scaffold to design compounds that inhibit specific biological targets [11,12,13], as well as for the synthesis of chemical libraries to be used in the Molecular Libraries Screening Center Network (MLSCN) screening effort
Summary
Small molecule biological probes that influence protein function are useful tools for studying the cell and can serve as lead structures in the development of new therapeutic agents [1,2,3,4,5]. Library substituted with two α-amino acid esters.
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