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Biologically Active Nuclear-Substituted Sulfonamides*: II. Bacteriostatic and Biological Activity of Some Nuclear-Substituted Sulfathiazoles

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Abstract

Seven new nuclear-substituted sulfathiazole derivatives were tested in uitro against Pastewella estis and Bacillus subtilis, and were compared with sulfathiazole and sulfanilamife in the presence and absence of para-aminobenzoic acid (PAB) by using a broth dilution method. Each of the nuclear-substituted sulfonamides was at least as active or more active than the parent compound, sulfathiazole. In in uiuo experiments, however, they were not superior to sulfathiazole in the therapy of either plague, staphylococcus, or streptococcus infection in the mouse. Generally, I these compounds are more toxic than sulfathiazole. Since the antibacterial activity of these nuclear-substituted derivatives is antagonized by p-aminobenzoic acid, they conform to the accepted definition of a true sulfanilamide-type compound. On the other hand, two thiophene sulfonamides tested were active antibacterial agents, but they were not inactivated' by PAB. The activity of these nuclear-substituted derivatives modifies some of the current concepts with regard to the relationship between the sulfanilamide structure and antibacterial activity.

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Fellow of the American Foundation for Pharmaceutical Education 1947-1950.

University of California College of Pharmacy. Professor of Pharmaceutical Chemistry.

§

George Williams Hooper Foundation for Medical Research, University of California Medical Center, San Francisco 22, Calif.

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