Abstract
AbstractThe preparation and biological evaluation of 7β‐[[2‐(phenyl)thiazol‐4‐yl]acetamido]cephalosporins and 7β‐[[(2‐(pyridin‐2‐yl)thiazol‐4‐yl]acetamido]cephalosporins, 9a‐o, substituted at the 3‐position with acetyloxymethyl, chlorine, hydrogen, and methyl are described. Hantzsch's thiazole synthesis is employed to provide thiazoleacetic acids 5a‐e, subsequently followed by Morpho CDI‐assisted amidation to complete the synthesis of target cephalosporins 9a‐o. These compounds display activity selectively against Gram‐positive bacteria, but are inactive against most Gram‐negative bacteria tested. Those with acetyloxymethyl at the 3‐position, i.e., 9a, 9e, 9i, 9m, and 90, exhibit activity with minimal inhibitory concentrations of 16 (μg/mL or lower against four strains of methicillin‐resistant staphylococci, namely Staphylococcus aureus X400 and S13E and Staphylococcus epidermidis 270 and 222. Notably, 9a displays an activity profile similar to that of vancomycin regarding its spectrum and potency.
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