Morata-Moreno Noelia, Pérez-Tanoira Ramón, Del Campo-Balguerias Almudena, Carrillo-Hermosilla Fernando, Hernando-Gozalo Marcos, Rescalvo-Casas Carlos, Ocana Ana V, Segui Pedro, Alonso-Moreno Carlos, Pérez-Martínez Francisco C, Molina-Alarcón Milagros
Department of Otorrinolaringology, Complejo Hospitalario Universitario, 02006 Albacete, Spain.
Departamento de Microbiología Clínica, Hospital Universitario Príncipe de Asturias, 28805 Madrid, Spain.
Antibiotics (Basel). 2024 Jun 29;13(7):609. doi: 10.3390/antibiotics13070609.
The guanidine core has been one of the most studied functional groups in medicinal chemistry, and guanylation reactions are powerful tools for synthesizing this kind of compound. In this study, a series of five guanidine-core small molecules were obtained through guanylation reactions. These compounds were then evaluated against three different strains of , one collection strain from the American Type Culture Collection (ATCC) of ATCC 35218, and two clinical extended-spectrum beta-lactamase (ESBL)-producing isolates (ESBL1 and ESBL2). Moreover, three different strains of were studied, one collection strain of ATCC 27853, and two clinical multidrug-resistant isolates (PA24 and PA35). Among Gram-positive strains, three different strains of , one collection strain of ATCC 29213, and two clinical methicillin-resistant (MRSA1 and MRSA2) were evaluated. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) experiments were reported, and the drop plate (DP) method was used to determine the number of viable suspended bacteria in a known beaker volume. The results from this assessment suggest that guanidine-core small molecules hold promise as therapeutic alternatives for treating infections caused by clinical Gram-negative and Gram-positive bacteria, highlighting the need for further studies to explore their potential. The results from this assessment suggest that the chemical structure of CAPP4 might serve as the basis for designing more active guanidine-based antimicrobial compounds, highlighting the need for further studies to explore their potential.
胍核心一直是药物化学中研究最多的官能团之一，胍基化反应是合成这类化合物的有力工具。在本研究中，通过胍基化反应获得了一系列五个胍核心小分子。然后针对三种不同的菌株对这些化合物进行了评估，一种是来自美国典型培养物保藏中心（ATCC）的保藏菌株ATCC 35218，以及两种临床产超广谱β-内酰胺酶（ESBL）的分离株（ESBL1和ESBL2）。此外，还研究了三种不同的菌株，一种是ATCC 27853的保藏菌株，以及两种临床多重耐药分离株（PA24和PA35）。在革兰氏阳性菌株中，评估了三种不同的菌株，一种是ATCC 29213的保藏菌株，以及两种临床耐甲氧西林金黄色葡萄球菌（MRSA1和MRSA2）。报告了最低抑菌浓度（MIC）和最低杀菌浓度（MBC）实验，并使用倾注平板（DP）法测定已知烧杯体积中存活悬浮细菌的数量。该评估结果表明，胍核心小分子有望成为治疗临床革兰氏阴性和革兰氏阳性细菌引起的感染的治疗替代品，突出了进一步研究以探索其潜力的必要性。该评估结果表明，CAPP4的化学结构可能作为设计更具活性的胍基抗菌化合物的基础，突出了进一步研究以探索其潜力的必要性。
