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ID: ALA1145884

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological activity of novel 1beta-methylcarbapenems with oxyiminopyrrolidinylamide moiety.

Authors: Lee JH, Lee KS, Kang YK, Yoo KH, Shin KJ, Kim DC, Kong JY, Lee Y, Lee SJ, Kim DJ.

Abstract: The synthesis and antibacterial activity of novel 1beta-methylcarbapenems 1a-f bearing oxyiminopyrrolidinylamide moiety at C-5 position of pyrrolidine are described. Most compounds exhibited comparable antibacterial activity to meropenem against a wide range of Gram-positive and Gram-negative organisms including Pseudomonas aeruginosa isolates. Of these carbapenems, 1a showed potent and broad spectrum of antibacterial activity and similar stability to DHP-I to meropenem. Against clinical isolates of 40 Gram-negative bacterial species including MDR and ESBL-producing strains, the selected carbapenem 1a possessed excellent in vitro activity except for MDR P. aeruginosa, and was comparable in potency to meropenem.

CiteXplore: 14643334

DOI: 10.1016/j.bmcl.2003.09.039