半合成β-ラクタム抗菌剤(第5報)6-[(R)-2-[3-(3,4-Dihydroxybenzoyl)-3-(3-hydroxypropyl)-1-ureido]-2-phenylacetamido]penicillanic Acid(AO-1100)のin Vitroにおける代謝とその代謝産物に関する研究

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Metabolism of 6-[(R)-2-[3-(3,4-dihydroxybenzoyl)-3-(3-hydroxypropyl)-1-ureido]-2-phenylacetamido] penicillanic acid (AO-1100), a new ureidopenicillin having catechol moiety, was studied in vitro, using catechol-O-methyltransferase (COMT) prepared from the rat and rabbit livers. Main two metabolites were detected by means of high performance liquid chromatography and identified as the monomethyl derivatives (M1,M2) of AO-1110 by the total synthesis. It was found that AO-1100 was metabolized easily by COMT prepared from the rat liver, and not easily by COMT from the rabbit liver. The metabolites (M1,M2) showed greatly reduced antibacterial activity against gram-negative bacteria including Pseudomonas aeruginosa.
社団法人日本薬学会の論文
1987-10-25