Korean Journal of Microbiology (미생물학회지)

The Microbiological Society of Korea (한국미생물학회)
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A study on the Synthesis and Biological Activity of Nucleoside Chemotherapeutic Agents

핵산계 화학요법제의 합성 및 생물활성에 관한 연구

  • 강신원 (부산대학교 자연과학대학 화학과) ;
  • 김경희 (부산대학교 자연과학대학 화학과) ;
  • 신정희 (부산대학교 자연과학대학 화학과) ;
  • 이봉헌 (부산대학교 자연과학대학 화학과) ;
  • 장태식 (부산대학교 자연과학대학 화학과)
  • Published : 1991.12.01
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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/sub 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/sub 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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