Chemical modification of penicillin β-lactam ring was made.Six thiazolidine amides were produced through N4-C7 β-lactam ring opening of penicillin V methyl ester with various aliphatic,aromatic,and heterocyclic prim...Chemical modification of penicillin β-lactam ring was made.Six thiazolidine amides were produced through N4-C7 β-lactam ring opening of penicillin V methyl ester with various aliphatic,aromatic,and heterocyclic primary amines.Five 8-hydroxypenillic acid derivatives with side chains of methyl,propyl,benzyl,and diethylaminoethyl groups were yielded via β-lactam ring rearrangement from6-aminopenicillanic acid（6-APA）.Parallel synthetic methods were used for the alkylation of8-hydroxypenillic acid and β-lactam ring opening of penicillin V methyl ester.The biological activities of the compounds were evaluated.展开更多
文摘Chemical modification of penicillin β-lactam ring was made.Six thiazolidine amides were produced through N4-C7 β-lactam ring opening of penicillin V methyl ester with various aliphatic,aromatic,and heterocyclic primary amines.Five 8-hydroxypenillic acid derivatives with side chains of methyl,propyl,benzyl,and diethylaminoethyl groups were yielded via β-lactam ring rearrangement from6-aminopenicillanic acid（6-APA）.Parallel synthetic methods were used for the alkylation of8-hydroxypenillic acid and β-lactam ring opening of penicillin V methyl ester.The biological activities of the compounds were evaluated.
