■本研究调查了十二种实验设计的C-2季吲哚酮对Providenciaspp的潜在生物活性。,已知引起尿路感染的肠杆菌科细菌。该研究旨在提供对所研究化合物的生物活性特性及其在开发针对Providenciaspp的新型治疗方法中的潜在用途的见解。吲哚啉酮的实验设计,结合其独特的化学结构,使他们有吸引力的候选人进一步调查。这项研究的结果可能有助于开发新的治疗剂来对抗Providenciaspp。感染。
■对合成的吲哚啉酮(moL1-moL12)进行评估,以确定任何优异的活性,特别关注拥有aza功能的moL12。所有12种化合物的抗微生物活性均针对六种不同的革兰氏阳性和革兰氏阴性生物体进行了一式三份测试。包括P.vermicola(P<0.05)。计算方法已用于评估化合物的药代动力学性质。
■在合成的吲哚啉酮中,moL12与具有相似骨架但不同功能部分的其他化合物相比表现出优异的活性。测试了所有六个菌株,包括P.vermicola,表现出对moL12的敏感性。计算研究支持moL12的药代动力学特性,表明可接受的吸收,分布,新陈代谢,排泄,和毒性特征。
■利用PPI方法,我们已经确定了一个有希望的目标,FabD,在革兰氏阴性细菌中。我们的分析表明,moL12在与FabD结合方面表现出显著的潜力,因此,可能会抑制细胞壁的形成,与其他化合物比拟,显示出优越的抗菌活性。因此,moL12可能是一种潜在的治疗剂,可用于抵抗由Providenciaspp引起的尿路感染。这项研究的结果为开发新的有效的细菌感染治疗方法提供了重要的前景。
UNASSIGNED: The present study investigates the potential bioactivity of twelve experimentally designed C-2 quaternary indolinones against Providencia spp., a bacterial group of the Enterobacteriaceae family known to cause urinary tract infections. The study aims to provide insights into the bioactive properties of the investigated compounds and their potential use in developing novel treatments against Providencia spp. The experimental design of indolinones, combined with their unique chemical structure, makes them attractive candidates for further investigation. The results of this research may contribute to the development of novel therapeutic agents to combat Providencia spp. infections.
UNASSIGNED: The synthesized indolinones (moL1-moL12) are evaluated to identify any superior activity, particularly focusing on moL12, which possesses aza functionality. The antimicrobial activities of all twelve compounds are tested in triplicates against six different Gram-positive and Gram-negative organisms, including P. vermicola (P<0.05). Computational methods have been employed to assess the pharmacokinetic properties of the compounds.
UNASSIGNED: Among the synthesized indolinones, moL12 exhibits superior activity compared to the other compounds with similar skeleton but different functional moieties. All six strains tested, including P. vermicola, demonstrated sensitivity to moL12. Computational studies support the pharmacokinetic properties of moL12, indicating acceptable absorption, distribution, metabolism, excretion, and toxicity characteristics.
UNASSIGNED: Utilizing the PPI approach, we have identified a promising target, FabD, in Gram-negative bacteria. Our analysis has shown that moL12 exhibits significant potential in binding with FabD, thereby, might inhibit cell wall formation, and display superior antimicrobial activity compared to other compounds. Consequently, moL12 may be a potential therapeutic agent that could be used to combat urinary tract infections caused by Providencia spp. The findings of this research hold significant promise for the development of new and effective treatments for bacterial infections.