ALKYL ETHER ANALOGS OF THE FK-506 RELATED, IMMUNOSUPPRESSIVE MACROLIDE L-683,590 (ASCOMYCIN)

被引:13
作者
GOULET, MT [1 ]
HODKEY, DW [1 ]
STARUCH, MJ [1 ]
DUMONT, FJ [1 ]
CRYAN, JG [1 ]
PARSONS, WH [1 ]
WYVRATT, MJ [1 ]
机构
[1] MERCK & CO INC,MERCK SHARP & DOHME RES LABS,DEPT IMMUNOL,RAHWAY,NJ 07065
关键词
D O I
10.1016/S0960-894X(01)80264-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
C32-O-Ether derivatives of L-683,590 have been prepared by alkylation with various alkyl, alkenyl, and alkynyl 2,2,2-trichloroacetimidates. These analogs exhibit good immunosuppressive activity in vitro, as measured in a T cell proliferation assay. In the case of cinnamyl ethers, this activity correlates with the lipophilicity (pi value) of the aromatic substituents.
引用
收藏
页码:921 / 926
页数:6
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