Antimalarial activity of N6-substituted adenosine derivatives (Part 2)

被引：26

作者：

Herforth, C

Wiesner, J

Franke, S

Golisade, A

Jomaa, H

Link, A

机构：

[1] Univ Hamburg, Fachbereich Chem, Inst Pharm, D-20146 Hamburg, Germany

[2] Jomaa Pharmaka GmbH, D-35392 Giessen, Germany

[3] Univ Hamburg, Fachbereich Chem, Inst Organ Chem, D-20146 Hamburg, Germany

来源：

JOURNAL OF COMBINATORIAL CHEMISTRY | 2002年 / 4卷 / 04期

关键词：

D O I：

10.1021/cc0100823

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

We have investigated the in vitro antimalarial activity of a new series of adenosine derivatives. The results show that N-6-(1-naphthylmethyl)-5'-deoxy-5'-(amido)adenosines as well as N-6-(4-phenylbenzyl)-5'-deoxy-5'-(amido)adenosines display significant activity against the malaria-causing parasites, with the sterically demanding bisubstituted species reported being active in most cases in the low-micromolar range. The novel compounds with unusual substitution pattern were obtained applying an efficient convergent polymer-assisted solution-phase (cPASP) synthesis protocol. Thus, we were able to prepare a series of substituted derivatives in parallel that would have been difficult to synthesize by standard techniques. The scope and limitations of the synthetic methodology are discussed.

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页码：302 / 314

页数：13

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