누클레오시드 유도체의 약품 구상 , 합성 및 생리 활성 연구

문성환; 김종안; 김경희; 구자석; 허남원; 김동규; 신홍대; 강신원

생화학분자생물학회 BMB Reports 누클레오시드 유도체의 약품 구상 , 합성 및 생리 활성 연구

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Nucleoside Derivatives ( 1 ) Synthesis and Biological Activity of Uridine Conjugates of Penicillin G and Peptides

문성환 , 김종안 , 김경희 , 구자석 , 허남원 , 김동규 , 신홍대 , 강신원 ( Sung Hwan Moon , Jong Ahn Kim , Keung Hee Kim , Ja Seok Koo , Nam Won Huh , Dong Kyu Kim , Hong Dae Shin , Shin Won Kang )

생화학분자생물학회 1987.01

BMB Reports vol. 20 iss. 4 345-349(5pages)

UCI I410-ECN-0102-2008-470-002212057

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Abstract

Six new uridine-conjugates of penicillin G and peptides have been prepared and evaluated against mouse lymphoblastoma L5178Y cells, Staphylococcus aureus(IAM 3610) and Escherichia coli (ATCC 10536). These include 5`-amino-5`-deoxyuridine-penicillin G(14), 5`-amino-5`-deoxyuridine-cyclo(Phe-Asp)(15-I), 5`-amino-5`-deoxyuridine-cyclo (Phe-Glu)(15-II), 5-iodo-5`-amino-2`,3`-0-isopropylidene uridine-penicillin G(16), 5-iodo-5`-amino-5`-deoxyuridine-penicillin G(17), and 5`-deoxyuridine-penicillin G(19). IC_(50) values were 18.0 ㎍/㎖, 6.5 ㎍/㎖, 6.5 ㎍/㎖, 13.5 ㎍/㎖, 6.5 ㎍/㎖ and 9.0 ㎍/㎖, respectively. MIC values of (15-I) and (17) were 6.25 ㎍/㎖. These preliminary results support the thesis that the uridine conjugates of this type may require a naturally occuring moiety for improved efficacy.

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