New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity

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• 作者：Johanna Faist^a ; ^{johanna.faist@uni-graz.at} ; Clemens Hinteregger^a ; Werner Seebacher^a ; Robert Saf^b ; Pascal Mä ; ser^c ; Marcel Kaiser^c ; Robert Weis^a
• 关键词：Amines ; Antiplasmodial activity ; Heterocycles ; NMR spectroscopy ; Nucleophilic substitutions ; Quinoline
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：25
• 期：3
• 页码：941-948
• 全文大小：363 K
• 卷排序：25

文摘

Novel ω-aminoacyl and -alkyl derivatives of 7-chloroquinolin-4-amine were prepared and their structures confirmed by NMR spectroscopy. Their antiprotozoal activities were examined in vitro against the sensitive NF54 strain as well as against the multiresistant K1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). The results were compared with the activities of clinically used drugs. Their antitrypanosomal activities were only moderate whereas their antiplasmodial activities looked very promising. Some were equal or slightly more active than chloroquine against the sensitive strain. However, in comparison to chloroquine, the activity of the new compounds was decreased much less in the resistant strain. Several possessed activity against both strains in low nanomolar concentration.