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

页码：3861 / 3865

页数：5

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