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基于噻唑的钴配合物作为新型群体感应淬灭剂、生物膜抑制剂和毒力减弱剂。

Cobalt Complex with Thiazole-Based Ligand as New Quorum Quencher, Biofilm Inhibitor and Virulence Attenuator.

机构信息

LEPABE, Department of Chemical Engineering, Faculty of Engineering, University of Porto, Rua Dr. Roberto Frias, s/n, Porto 4200-465, Portugal.

Faculty of Chemistry, University of Belgrade, Studentski trg 12⁻16, Belgrade 11000, Serbia.

出版信息

Molecules. 2018 Jun 8;23(6):1385. doi: 10.3390/molecules23061385.

DOI:10.3390/molecules23061385
PMID:29890626
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6099793/
Abstract

is one of the most dreaded human pathogens, because of its intrinsic resistance to a number of commonly used antibiotics and ability to form sessile communities (biofilms). Innovative treatment strategies are required and that can rely on the attenuation of the pathogenicity and virulence traits. The interruption of the mechanisms of intercellular communication in bacteria (quorum sensing) is one of such promising strategies. A cobalt coordination compound (Co()₂) synthesized from ()-2-(2-(pyridin-2-ylmethylene)hydrazinyl)-4-(p-tolyl)thiazole () is reported herein for the first time to inhibit 3-oxo-C12-HSL-dependent QS system (LasI/LasR system) and underling phenotypes (biofilm formation and virulence factors). Its interactions with a possible target, the transcriptional activator protein complex LasR-3-oxo-C12-HSL, was studied by molecular modeling with the coordination compound ligand having stronger predicted interactions than those of co-crystallized ligand 3-oxo-C12-HSL, as well as known-binder furvina. Transition metal group 9 coordination compounds may be explored in antipathogenic/antibacterial drug design.

摘要

铜绿假单胞菌是最可怕的人类病原体之一，因为它对许多常用抗生素具有固有耐药性，并且能够形成静止的群落（生物膜）。需要创新的治疗策略，这些策略可以依赖于降低致病性和毒力特征。中断细菌（群体感应）细胞间通讯的机制是一种很有前途的策略。本文首次报道了一种由（）-2-（2-（吡啶-2-亚甲基）肼基）-4-（对甲苯基）噻唑（）合成的钴配合物（Co()₂），用于抑制 3-氧代-C12-HSL 依赖性 QS 系统（LasI/LasR 系统）和潜在表型（生物膜形成和毒力因子）。通过分子建模研究了其与可能的靶标，即转录激活蛋白复合物 LasR-3-氧代-C12-HSL 的相互作用，预测配合物配体的相互作用比共结晶配体 3-氧代-C12-HSL 以及已知结合物 furvina 更强。过渡金属第 9 族配合物可用于抗病原体/抗菌药物设计。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/b0b08cd5364e/molecules-23-01385-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/8cd5929a846c/molecules-23-01385-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/e4997940bfc7/molecules-23-01385-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/f6de273cd9bc/molecules-23-01385-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/25b49e7de15a/molecules-23-01385-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/36085040135b/molecules-23-01385-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/88e610b652ce/molecules-23-01385-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/a3e6c7459e5f/molecules-23-01385-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/b0b08cd5364e/molecules-23-01385-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/8cd5929a846c/molecules-23-01385-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/e4997940bfc7/molecules-23-01385-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/f6de273cd9bc/molecules-23-01385-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/25b49e7de15a/molecules-23-01385-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/36085040135b/molecules-23-01385-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/88e610b652ce/molecules-23-01385-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/a3e6c7459e5f/molecules-23-01385-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0242/6099793/b0b08cd5364e/molecules-23-01385-g007.jpg

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