Abstract

Structure-activity relationships were examined for a number of α-sulfopenicillins and related compounds. Among the α-sulfopenicillins tested, the α-thienyl and α-(p-aminophenyl) homologues showed the greatest activity against Pseudomonas aeruginosa, and broad spectra comparable to that of α-sulfobenzylpenicillin (1). With the exception of these two homologues, any modification in position or structure of the α-sulfo or α-phenyl group of 1, diminished activity. Relationships between antipseudomonal or antistaphylococcal activity and a negative charge in the acyl side chain are discussed.

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