Synthesis and biological evaluation of non-peptidic cyclophilin ligands

被引：22

作者：

Wu, YQ ^{[1
]}

Belyakov, S ^{[1
]}

Choi, C ^{[1
]}

Limburg, D ^{[1
]}

Thomas, BE ^{[1
]}

Vaal, M ^{[1
]}

Wei, L ^{[1
]}

Wilkinson, DE ^{[1
]}

Holmes, A ^{[1
]}

Fuller, M ^{[1
]}

McCormick, J ^{[1
]}

Connolly, M ^{[1
]}

Moeller, T ^{[1
]}

Steiner, J ^{[1
]}

Hamilton, GS ^{[1
]}

机构：

[1] Guilford Pharmaceut Inc, Dept Res, Baltimore, MD 21224 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 07期

关键词：

D O I：

10.1021/jm020409u

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Peptidylprolyl isomerase cyclophilins play critical roles in a variety of biological processes. Recent findings that cyclophilins are present at high levels in the CNS and that cyclosporin A may possess neuroprotective/neurotrophic effects have prompted us to search for nonimmunosuppressant small molecule cyclophilin ligands. To this end, we report the lead identification through "virtual screening" and the synthesis of our first series of non-peptidic cyclophilin ligands, along with the preliminary biological results.

引用

页码：1112 / 1115

页数：4

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