A concise synthesis and antimicrobial activities of 3-polyamino-23,24-bisnorcholanes as steroid-polyamine conjugates

被引：9
作者：
Kim, Hong-Seok [1 ]
Khan, Sharaf N. [1 ]
Jadhav, Jyoti R. [1 ]
Jeong, Ji-Woong [2 ]
Jung, Kyungjin [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
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 13期
关键词：
Steroid-polyamine conjugate; SAR; Reductive amination; Antimicrobial activity; STEREOSELECTIVE-SYNTHESIS; REDUCTIVE AMINATION; 2-DIMENSIONAL NMR; FORMAL SYNTHESIS; POLYMYXIN-B; SQUALAMINE; DNA; DESIGN; ANTIBIOTICS; DERIVATIVES;
D O I：
10.1016/j.bmcl.2011.05.048
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of steroid-polyamine conjugates were synthesized and evaluated for their antimicrobial activity. This study was focused on the effect of stereochemistry at the C-3 and C-5 of steroids and types of polyamine at C-3 on activity against various human pathogens. All the conjugates exhibited strong antimicrobial activities against Gram-positive strains. Compound 18 was found to be the most potent in these series with a MIC value as low as 1 mu g/mL against the bacterium Staphylococcus aureus ATCC6538P. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3861 / 3865
页数：5
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