Unfused heterobicycles as amplifiers of phleomycin. III. Thiazolylpyridines and bipyrimidines with strongly basic side chains

Abstract

Syntheses are described for 4-(thiazol-4'-yl)pyridines, each 2'-substituted by a dialkylaminoalkyl, dialkylaminoalkylthio or dialkylaminoalkylamino side chain; for 2- and 3-(thiazol-4'-yl)pyridines with a 2'-dimethylaminoethylthio substituent; for 4-(thiazol-2'-yl)pyridines with either a 4'- or a 5'-dialkylaminoalkylcarbamoyl substituent; and for some analogous compounds. The above and similarly substituted 2,4'-, 4,5'- and 5,5'-bipyrimidines have been screened for activity as amplifiers of phleomycin-G against Escherichia coli B by an improved in vitro procedure. The results are tabulated and discussed.