Synthesis and antimicrobial activity of 3-aryl-4,5,6,7-tetrahydroindazoles

被引：3
|
作者：
Pantyukhin, A. A. [1 ]
Mikhailovskii, A. G. [1 ]
Aleksandrova, G. A. [2 ]
Makhmudov, R. R. [2 ]
Pershina, N. N. [1 ]
Vakhrin, M. I. [1 ]
机构：
[1] Perm State Pharmaceut Acad, Perm, Russia
[2] Perm State Univ, Inst Nat Sci, Perm, Russia
来源：
PHARMACEUTICAL CHEMISTRY JOURNAL | 2012年 / 46卷 / 08期
关键词：
1-piperidinocyclohexene; aroylchlorides; 2-aroylcyclohexanones; hydrazine hydrate; 3-aryl-4,5,6,7-tetrahydroindazoles; hydrochlorides; activity against Staphylococcus aureus and Candida albicans at concentrations 2 and 3.9 mu g/mL; respectively;
D O I：
10.1007/s11094-012-0827-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Acylation of 1-piperidinocyclohexene by aroylchlorides yielded 2-aroylcyclohexanones. The obtained 1,3-diketones reacted with hydrazine hydrate to yield 3-aryl-4,5,6,7-tetrahydroindazoles, which formed stable hydrochlorides showing a high level of activity against Staphylococcus aureus and Candida albicans. The maximum activity against the bacterial strain was observed for the compound containing a 4-bromophenyl radical (the inhibition and bactericidal effects were produced at concentrations of 2 and 7.8 mu g/mL, respectively). The maximum activity against the fungal strain was observed for the compound with a p-tolyl radical (the corresponding concentrations being 3.9 and 31.2 mu g/mL).
引用
收藏
页码：470 / 472
页数：3
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