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Synthesis of Substituted Imidazolidin-2-ones as Aminoacyl-tRNA Synthase Inhibitors

Substituted imidazolidin-2-ones deduced as potential inhibitors of IleRS by docking simulations were synthesized from aziridine-2-carboxaldehyde. Reductive amination of aziridine-2-carboxaldehyde with dipeptides for the substituents at N1 and followed by aziridine-ring expansion with triphosgene aff...

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Published in:Bulletin of the Korean Chemical Society 2010, 31(3), , pp.611-614
Main Authors: Eum, Hee-Sung, Lee, Yu-No, Kim, Song-Mi, Baek, A-Young, Son, Min-Ky, Lee, Keun-Woo, Ko, Seung-Whan, Kim, Sung-Hoon, Yun, Sae-Young, Lee, Won-Koo, Ha, Hyun-Joon
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Language:English
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Summary:Substituted imidazolidin-2-ones deduced as potential inhibitors of IleRS by docking simulations were synthesized from aziridine-2-carboxaldehyde. Reductive amination of aziridine-2-carboxaldehyde with dipeptides for the substituents at N1 and followed by aziridine-ring expansion with triphosgene afforded 4-chloromethylimidazolidin-2-one whose chloride were further manipulated towards phenylurea, pyrimidin-2-yl-urea or benzenesulfonamide at C4. KCI Citation Count: 6
ISSN:0253-2964
1229-5949
DOI:10.5012/bkcs.2010.31.03.611