Synthesis and in vitro activity of oleanolic acid derivatives against Chlamydia trachomatis and Staphylococcus aureus

被引：0
作者：
Oxana Kazakova
Liudmila Rubanik
Irina Smirnova
Nikolay Poleschuk
Anastasia Petrova
Yuliya Kapustsina
Irina Baikova
Elena Tret’yakova
Elmira Khusnutdinova
机构：
[1] Ufa Institute of Chemistry of the Ufa Federal Research Centre of the Russian Academy of Sciences,
[2] Republican Research and Practical Center for Epidemiology and Microbiology,undefined
来源：
Medicinal Chemistry Research | 2021年 / 30卷
关键词：
Triterpenoids; Oleanolic acid; Antimicrobial activity; NCI-60;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A series of nitrogen-containing modificants with amide, arylidene or heterocyclic fragments of oleanolic, oleanonic and 2,3-indolo-oleanolic acids have been synthesized and evaluated for activity against C. trachomatis and key ESKAPE pathogens. Oleanolic acid conjugates with homopyperazine 3, N-hydroxymethyl-homopyperazine 4, and diethylenetriamine 23 demonstrated a high inhibitory activity against C. trachomatis with chemotherapeutic index (CTI) 8 and >8, while 3-amino-3,4-seco-4(23)-en-erythrodiol 22 was found to be a leader compound with significant activity (MIC 3.125 μg/mL). Compounds 3 and 22 showed a moderate activity against MRSA with MICs of 8 and 4 μg/mL. Compounds 2, 3, and 23 exhibited remarkable activities against NCI-60 subpanel (GI50 ranges from 0.18 to 2.21 μM) exceeding the activity of sorafenib with compound 23 as a leader (GI50 0.17 μM for melanoma LOX IMVI).
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页码：1408 / 1418
页数：10
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