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5-Carboxamido-4-amino-3-isoxazolidone, and asparagine analogue.

作者信息

Stammer C H, Sato M

出版信息

J Med Chem. 1978 Jul;21(7):709-12. doi: 10.1021/jm00205a026.

Abstract

trans-Aziridine-2,3-dicarboxylic ester was used to prepare the required beta-chlorohydroxamic acid used in the synthesis of the title compound. The trans configuration of the asparagine analogue was established by hydrogenolysis to erythro-beta-hydroxyasparagine amide. Neither the title compound nor the intermediate aziridinehydroxamic acid (8) showed significant activity against the L1210 and P-388 tumors. The title compound was inactive as an inhibitor of asparagine synthetase from Novikoff hepatoma and did not inhibit the growth of some 25 bacteria and fungi.

摘要

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