POLYCYCLIC AROMATIC ALKALOIDS .10. ANNONACEOUS ALKALOIDS WITH ANTIFUNGAL ACTIVITY

被引：37

作者：

BRACHER, F

机构：

[1] Institut für Pharmazeutische Chemie der Technischen Universität, Braunschweig, D-38106

来源：

ARCHIV DER PHARMAZIE | 1994年 / 327卷 / 06期

关键词：

D O I：

10.1002/ardp.19943270605

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Two strategies towards the synthesis of isomerically pure azafluorenones are described. Cyclization of the aryl nicotinic acid 7 with polyphosphoric acid and subsequent reductive debromination gives 8-methoxyonychine (3) (''method A''). 6-Methoxyonychine (2), an alkaloid from annonaceae, can be prepared by Parham-cyclization of the carboxylic acid 7 or of the ester 6 (''method B''), In an agar-well diffusion assay 2, 3, and onychine (9a) show moderate activity against Candida albicans. 9e has stronger activity, while other azafluorenones are almost inactive. The structurally related azaoxoaporphine alkaloid sampangine (12) has very strong antifungal activity.

引用

页码：371 / 375

页数：5

共 21 条

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[2]

POLYCYCLIC AROMATIC ALKALOIDS .7. STUDIES ON THE STRUCTURE OF DIELSINE [J].