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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 07期

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

页码：921 / 926

页数：6

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