Synthesis and antimicrobial activity of imidazole and pyridine appended cholestane-based conjugates

被引:39
作者
Kim, Hong-Seok [1 ]
Jadhav, Jyoti R. [1 ]
Jung, Sung-Ji [2 ]
Kwak, Jin-Hwan [2 ]
机构
[1] Kyungpook Natl Univ, Dept Appl Chem, Taegu 702701, South Korea
[2] Handong Global Univ, Sch Life Sci, Pohang 791708, South Korea
关键词
Cholestane; Imidazole; Pyridine; Antimicrobial activity; RESISTANT STAPHYLOCOCCUS-AUREUS; ANTIINFLAMMATORY ACTIVITIES; DERIVATIVES; SQUALAMINE; DESIGN; ANTIBIOTICS; ANTIFUNGAL; PEPTIDES; BACTERIA; AGENTS;
D O I
10.1016/j.bmcl.2013.05.098
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 3 alpha-amino-5 alpha-cholestane and 3 alpha,7 alpha-diamino-5 alpha-cholestane derivatives containing imidazole and pyridine rings were synthesized by simple and effective reductive amination, and their in vitro activities against a range of Gram-positive and Gram-negative strains were evaluated. Most of the compound exhibited enhanced activity against MRSA pathogen. 3 alpha,7 alpha-Di(pyridylmethyl)amino-5 alpha-cholestane 10 showed the highest potency in these series toward the Gram-positive bacteria, Staphylococcus epidermidis 887E, with the lowest MIC value of 1 mu g/mL. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4315 / 4318
页数:4
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