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用于抗菌和抗肿瘤活性的苄基芴基及1-芳基乙基季铵盐的合成与评价

Synthesis and evaluation of benzylfluorenyl and 1-arylethyl quaternary ammonium salts for antimicrobial and antineoplastic activities.

作者信息

Dimmock J R, Smith P J, Tsui S K

出版信息

J Pharm Sci. 1979 Jul;68(7):866-71. doi: 10.1002/jps.2600680721.

Abstract

A number of substituted benzyldimethyl-9-fluorenylammonium bromides (II) and 9-benzylfluorenyl-9-trimethylammonium bromides (IV) were synthesized and examined for antimicrobial and anticancer activites. Series IV showed greater antimicrobial activity than Series II while some corresponding acyclic fluorene analogs were bereft of antimicrobial activities. Significant antineoplastic activity was not found in Series II and IIV. Representative fluorenes subjected to a preliminary screen for various pharmacological activities revealed marked anti-inflammatory and analgesic properties coupled with some antihistaminic activities. The acyclic quaternary ammonium compounds demonstrated substantial pressor activites.

摘要

合成了多种取代苄基二甲基 - 9 - 芴基溴化铵(II)和9 - 苄基芴基 - 9 - 三甲基溴化铵(IV),并对其抗菌和抗癌活性进行了检测。系列IV显示出比系列II更强的抗菌活性,而一些相应的无环芴类似物则没有抗菌活性。在系列II和IV中未发现显著的抗肿瘤活性。对代表性芴进行的各种药理活性初步筛选显示出明显的抗炎和镇痛特性以及一些抗组胺活性。无环季铵化合物表现出显著的升压活性。

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