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Synthesis of desaza analogues of annomontine and canthin-4-one alkaloids.

作者信息

Strödke Benjamin, Gehring André P, Bracher Franz

机构信息

Department of Pharmacy - Center for Drug Research, Ludwig-Maximilians-University of Munich, Munich, Germany.

出版信息

Arch Pharm (Weinheim). 2015 Feb;348(2):125-31. doi: 10.1002/ardp.201400328.

DOI:10.1002/ardp.201400328
PMID:25664630
Abstract

1-Acetylcarbazoles are readily converted to 3-desazacanthin-4-ones upon treatment with Bredereck's reagent, but in contrast to canthin-4-ones, these do not undergo ring transformation reactions with guanidine. Only after N-protection (methyl or 2-(trimethylsilyl)ethoxymethyl group), 2-desaza analogues of the alkaloid annomontine are accessible via the enaminoketones obtained by condensation with Bredereck's reagent. One of the annomontine analogues is an inhibitor of the Plasmodium falciparum CDC-like kinases (CLK) and shows antimalarial activity.

摘要

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