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具有抗菌活性的小分子两亲性肽树状大分子的设计。

Design of antimicrobially active small amphiphilic peptide dendrimers.

机构信息

Institute of Organic Chemistry PAS, Kasprzaka Str. 44/52 01-224 Warsaw, Poland.

出版信息

Molecules. 2009 Sep 29;14(10):3881-905. doi: 10.3390/molecules14103881.

Abstract

Novel polyfunctional small amphiphilic peptide dendrimers characterized by incorporation of a new core compounds - tris-amino acids or tetrakis-amino alcohols that originated from a series of basic amino acids - were efficiently synthesized. These new core elements yielded molecules with multiple branching and (+5)/(+6) charge at the 1-st dendrimer generation. Dendrimers exhibited significant antimicrobial potency against Gram(+) and Gram(-) strains involving also multiresistant reference strains (S. aureus ATCC 43300 and E. coli ATCC BAA-198). In addition, high activity against fungi from the Candida genus was detected. More charged and more hydrophobic peptide dendrimers expressed hemolytic properties.

摘要

新型多功能小分子两亲性肽树状聚合物的特点是引入了新的核心化合物——三氨基酸或四氨基酸醇,它们来源于一系列碱性氨基酸。这些新的核心元素生成了具有多个分支和(+5)/(+6)电荷的分子,位于第一代树状聚合物上。树状聚合物对革兰氏阳性和革兰氏阴性菌株表现出显著的抗菌效力,同时也对多药耐药参考菌株(金黄色葡萄球菌 ATCC 43300 和大肠杆菌 ATCC BAA-198)有效。此外,还检测到对念珠菌属真菌的高活性。带更多电荷和疏水性的肽树状聚合物表现出溶血特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f07/6255327/2df85859601e/molecules-14-03881-g003.jpg

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