Title 핵산계 화학요법제의 합성 및 생물활성에 관한 연구
Author 강신원 · 김경희 * · 신정희 · 이봉헌 · 장태식
Address 부산대학교 자연과학대학 화학과
Bibliography Korean Journal of Microbiology, 29(6),353-360, 1991
Key Words Nucleoside, biological activity, Chemotherapeutic agent, Uridine 5'-monophosphate
Abstract 5-substituted uridine(I,Br,Cl), 5'-amino-5'-deoxyuridine conjugates of amino acid, peptide and penicillin G, 5'-monophosphate uridine derivatives and 5'-monophosphate-fatty acid detrivatives were chemically synthesized. Their biological activities were determined as MIC and IC_50 unit against various pathogenic microorganisms in vitro. 5'-amino-5'-deoxyuridine-cyclo(Phe-Asp)(23), 5-iodo-5'-amino-deoxyuridine-penicillin G(26) were the most efficient; their IC_50 against L5178Y murine lymphoma cell was 6.5 h/ml, MIC against S. aureus (+) and E. coli (-) was 6.25 g/ml. MIC of 5-bromo-2', 3'-O-isopropylideneuridine(6) against Trichophyton rubrum was 0.2 g/ml. And 5'-monophosphate derivatives are more active than simple uridine derivatives, suggesting other modified nucleoside 5'-phosphate may be worthwhile examing further as a new prodrugs.
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