Ampicillin及びAmoxicillin誘導体の研究(第3報)6-[2-[(Pyrido[2,3-d]pyrimidin-6-yl)methylamino]-2-phenylacetamido]penicillanic Acid誘導体, 6-[2-(4-Pyrimidinylamino)-2-phenylacetamido]penicillanic Acid誘導体及び-cephalosporanic Acid誘導体の合成

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A series of N-alkylampicillin (2), N-heteroarylampicillin (5) and N-heteroarylcephalexin (6) were synthesized in order to obtain β-lactam detivatives with a broad and orallypotent antibacterial activity similar to that of the injectable N-acylampicillins. 6-[2-[(Pyrido [2,3-d] pyrimidin-6-yl) methylamino]-2-phenylacetamido] penicillanic acid derivatives (2) were prepared by the reduction of the Schiff base which was derived from the reaction of pyrido [2,3-d] pyrimidine-6-carboxaldehyde (1) with ampicillin. 6-N-(4-Pyrimidinyl) ampicillin and -cephalexin derivatives (5 and 6) were obtained by the reaction of 4-chloropyrimidine (4) with ampicillin or cephalexin. Compounds 2,5 and 6 were tested in vitro antibacterial activity and, however, none of them have a broad and potent activity.
公益社団法人日本薬学会の論文
1987-08-25