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A series of 8-alkyl-2-amino (or substituted-amino)-5, 8-dihydro-5-oxopyrido [2, 3-d]-pyrimidine-6-carboxylic acids and related compounds were synthesized and evaluated as antibacterial agents. The most active compounds in vitro against Escherichia coli and Staphylococcus aureus were 8-ethyl-5, 8-dihydro-2-dimethylamino-5-oxopyrido [2, 3-d]-pyrimidine-6-carboxylic acid (VII a) and 8-ethyl-5, 8-dihydro-5-oxo-2-pyrrolidinopyrido-[2, 3-d] pyrimidine-6-carboxylic acid, piromidic acid, (VIIb). Structure-activity relationships are discussed.
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MINAMI et al. (1971) studied this question.