Pyrazole derived ultra-short antimicrobial peptidomimetics with potent anti-biofilm activity

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• 作者：Mija Ahn^a ; ¹ ; Pethaiah Gunasekaran^b ; ¹ ; Ganesan Rajasekaran^c ; ¹ ; Eun Young Kim^c ; ¹ ; Soo-Jae Lee^d ; Geul Bang^e ; Kun Cho^e ; Jae-Kyung Hyun^f ; Hyun-Ju Lee^f ; ^g ; Young Ho Jeon^h ; Nam-Hyung Kim^b ; Eun Kyoung Ryu^a ; ⁱ ; Song Yub Shin^c ; ^{syshin@chosun.ac.kr} ; Jeong Kyu Bang^a ; ⁱ ; ^{bangjk@kbsi.re.kr}
• 关键词：Ultra-short peptidomimetics ; Pyrazole-derived amino acids ; Antimicrobial activity ; Anti-biofilm activity ; Bacterial killing mechanism
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：551-564
• 全文大小：1747 K
• 卷排序：125

文摘

Synthesis of Fmoc-pyrazole amino acids for the first time. Synthesis of Pyrazole-arginine based ultra short peptidomimetics using solid phase peptide synthesis. Ultra short peptidomimetics showed broad-spectrum of antimicrobial activity including MRSA, VREF, and MDRPA. Ultra short peptidomimetics also displayed potent anti-biofilm activity. Mechanistic studies including inner membrane, outer membrane permeability, membrane depolarization and TEM images.