Cefadroxil을 사용한 Alkylene Bisdithioureido $\beta$-Lactam 유도체의 합성 및 항균작용

The Synthesis and Antispectrum of Alkylene Bisthioureido $\beta$-tactam Derivatives of Cefadroxil.

Spanner chain의 탄소수가 2,4 또는 6개의 alkylene diisothiocyanate를 합성 후 cefadroxil-2DMF와 반응시켜 spanner chain의 탄소수 2, 4 또는 6개로 연결되어 있고 양쪽에 thioureido group과 $\beta$-lactam ring을 가진 bivalent ligand 구조의 alkylene bisdithioureido $\beta$-lactam 유도체를 합성하고 그 화합물들의 항균작용에 대하여 연구하였다. 그 유도체의 I식 화합물은 $C_{36}$H$_{38}$N$_{8}$O$_{10}$S$_4$, II식 화합물은 $C_{38}$H$_{42}$N$_{8}$O$_{10}$S$_4$, III식 화합물은 $C_{40}$H$_{46}$N$_{8}$O$_{10}$S$_4$의 분자식이다. $\beta$-lactam 감수성 균주에 대한 항균력은 spnner chain의 탄소수가 많을수록 감소하였다.

The three new Alkylene bisdithionreido $\beta$-lactam derivatives were synthesized and evaluated for antimicrobial activities. Treatment of cefadroxil.2DMF with alkylene diisothiocyanate which was obtained by the reaction of alkylene diamine with carbon disulfide, sodium hydroxide and ethyl chloroformate afforden alkylene bisdithioureido $\beta$ -lactam derivatiives. The antimicrobial activities of the compounds synthesized were ethylene bisdithioureido $\beta$-lactam derivative lost the sensitivity against Escherichia coli but showed potent antimicrobial activity against $\beta$-lactams Escherichia coli, but, tetramethylene bisdithioureido $\beta$-lactam derivative and hexamethylene bisdithioureido $\beta$ -lactam derivative compounds showed diminished or no antimicrobial activities.