POTENTIAL PRODRUGS OF 6-ACETYLMETHYLENEPENICILLANIC ACID (Ro 15-1903)
1986 年 39 巻 6 号 p. 833-838
詳細
1986 年 39 巻 6 号 p. 833-838
The synthesis and biological activities of a series of non-classical penicillins are described. These compounds were synthesized by treating the pivaloyloxymethyl ester of 6-acetylmethylenepenicillanic acid (Ro 15-1903) with various nucleophiles. They were found to be less active against the β-lactamases from Proteus vulgaris 1028, Escherichia coli1024, Klebsiella pneumoniaeNCTC 418 and E. coliRTEM than the parent compound. Nevertheless, synergy with ampicillin against whole bacterial cells producing β-lactamases was evident, although the single compounds did not exhibit antibacterial properties. With the compounds 2a and 2b, synergistic interaction with ampicillin could also be demonstrated in mice.
