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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 31, Number 3
BKCSDE 31(3)
March 20, 2010 

Synthesis of Substituted Imidazolidin-2-ones as Aminoacyl-tRNA Synthase Inhibitors
Heesung Eum, Yuno Lee, a Songmi Kim, Ayoung Baek, Minky Son, Keun Woo Lee, Seung Whan Ko, Sunghoon Kim, Sae Young Yun, Won Koo Lee, Hyun Joon Ha*
Aminoacyl-tRNA synthase inhibitors, Imidazolidin-2-ones
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.
611 - 614
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