• 약학회지
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• 제38권6호
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• pp.664-672
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• 1994

Eighteen new hybrid bivalent ligand quinolones that contain two different type of pharmacophores in a single molecule were prepared and evaluated for in viかo antibacterial activity. Hybrid bivalent ligands p-nitrobenzyloxycarbonyl quinolones were prepared by the treatment of active esters of succinyl fluoroquinolones with 1,7-disubstituted fluoroquinolone carboxylic acids in DMF. Eighteen final quinolone carboxylic acids were obtained by the reduction of compounds $25{\sim}42$ with hydrogen in the presence of 10% Pd-C. Among these derivatives, compound[56] showed the most potent antibacterial activity against a wide range of microoranisms.

• Biomolecules & Therapeutics
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• 제7권2호
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• pp.164-169
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• 1999

The synthesis and antimicrobial activity of N-substituted glycol derivatives of Norfloxacin were described. Norfloxacin was treated with chloroacetyl chloride to yield chloroacetyl norfloxacin (1). This compounds was reacted with alkyldiamines to afford bivalent ligand quinolone carboxylic acids (2-6), which was added to pivaloyloxymethyl chloride to give bivalent ligand pivaloyloxymethyl quinolone carboxylates (7-11). Chloroacetyl norfloxacin (1) treated with alkylamines to obtain monovalent ligand quinolone carboxylic acids (12-15), which was reacted with pivaloyloxymethyl chloride to get monovalent ligand pivaloyloxymethyl quinolone carboxylates (16-19). Free carboxylic quinolones (2-6, 12-15) showed little stronger activities to their pivaloyloxymethyl esters (7-11, 16-19). In monovalent ligand quinolone analogues, longer a1kyl chain com-pounds showed stronger activities than shorter one.

• 분석과학
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• 제8권4호
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• pp.449-456
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• 1995

Novel macrocyclic ligands modified with pendant arms, N, N', N'', N''', N'''', N'''''-hexakis(2-aminoethyl)-1, 4, 7, 10, 13, 16-hexaazacyclootadecane [$L_3$, Fig.1] and 1, 4, 7-tris(3-(o-hydroxyphenyl)propyl)-1, 4, 7-triazacyclononane [$L_4$, Fig.1] have been synthesized, and the protonation of $L_3$ and $L_4$ and stability constants of $L_3$ with bivalent transition metal ions and rare earth metal ions were determined by a potentiometry. The obtained results show that the complex formation of $L_3$ depends on the metal ligand ratios, and the stability of the metal complexes does not depend on the sizes of the metal ions, but on the nature of the metal ions. The structures of the rare earth complexes for $L_4$ were characterized by an X-ray absorption spectrometry(XAFS).

• 한국미생물·생명공학회지
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• 제17권3호
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• pp.193-197
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• 1989

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.