Synthesis of substituted imidazolidin-2-ones as aminoacyl-tRNA synthase inhibitors

Heesung Eum, Yuno Lee, Songmi Kim, Ayoung Baek, Minky Son, Keun Woo Lee, Seung Whan Ko, Sunghoon Kim, Sae Young Yun, Won Koo Lee, Hyun Joon Ha

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Abstract

Substituted imidazolidin-2-ones deduced as potential inhibitors of IleRS by docking simulations were synthesized from an aziridine-2-carboxaldehyde. Reductive amination of an aziridine-2-carboxaldehyde with dipeptides for the substituents at N1 and followed by aziridine-ring expansion with triphosgene afforded 4-chloromethylimidazolidin-2-ones whose chloride were further manipulated towards phenylurea, pyrimidin-2-yl-urea or benzenesulfonamide at C4.

Original languageEnglish
Pages (from-to)611-614
Number of pages4
JournalBulletin of the Korean Chemical Society
Volume31
Issue number3
DOIs
Publication statusPublished - 2010 Mar 1

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All Science Journal Classification (ASJC) codes

  • Chemistry(all)

Cite this

Eum, H., Lee, Y., Kim, S., Baek, A., Son, M., Lee, K. W., Ko, S. W., Kim, S., Yun, S. Y., Lee, W. K., & Ha, H. J. (2010). Synthesis of substituted imidazolidin-2-ones as aminoacyl-tRNA synthase inhibitors. Bulletin of the Korean Chemical Society, 31(3), 611-614. https://doi.org/10.5012/bkcs.2010.31.03.611