Journal
JOURNAL OF ANTIBIOTICS
Volume 53, Issue 11, Pages 1272-1281Publisher
JAPAN ANTIBIOT RES ASSN
DOI: 10.7164/antibiotics.53.1272
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The discovery of RWJ-54428 (MC-02,479), a new cephalosporin displaying promising activity against sensitive and resistant Gram-positive bacteria, is described. Progressive structural modification from the previously reported 3-phenylthiocephem MC-02,331 afforded an overall increase in potency against MRSA while retaining other key properties such as acceptable solubility and serum binding. Evaluation of the iii vitro potency and lit vivo efficacy of a series of closely related compounds resulted in selection of RWJ-54428 (MC-02,479) for further studies.
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