Monocyclic pteridine analogs. Inhibition of Escherichia coli dihydropteroate synthase by 6-amino-5-nitrosoisocytosines

…, LN Bell, HM McGuire, R Ferone

Index: Lever, O. William; Bell, Lawrence N.; McGuire, H. Michael; Ferone, Robert Journal of Medicinal Chemistry, 1985 , vol. 28, # 12 p. 1870 - 1874

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Citation Number: 26

Abstract

A variety of 5, 6-disubstituted isocytosine derivatives were evaluated in vitro as inhibitors of dihydropteroate synthase from Escherichia coli. A number of 6-(alkylamino)-5- nitrosoisocytosines have in vitro potency equivalent with or superior to that of therapeutically effective sulfonamide inhibitors of the synthase. The sulfonamide drugs are known to compete for the p-aminobenzoic acid binding site of the synthase, and kinetic analysis of ...