A New Discovery towards Novel Skeleton of Benzimidazole-Conjugated Pyrimidinones as Unique Effective Antibacterial Agents
作者机构：Institute of Bioorganic&Medicinal ChemistryKey Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing400715China College of PharmacyNational&Local Joint Engineering Research Center of Targeted and Innovative TherapeuticsChongqing Key Laboratoryof KinaseModulators as InnovativeMedicineChongqing University of Arts and SciencesChongqing 402160China
出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)
年 卷 期：2022年第40卷第22期
页 面：2642-2654页
核心收录：
学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学]
基 金：supported by grants from the National Natural Science Foundation of China(No.21971212) the Research Fellowship for International Young Scientists from International(Regional)-Cooperation and Exchange Program of China National Natural ScienceFoundation(No.81350110523) theKey Project of Innovation Research 2035Pilot Plan of Southwest University(SWU-XDZD22007)
主 题：Pyrimidinone Benzimidazole Antibacterial Resistance Membrane
摘 要：A class of new potential antibacterial agents with distinctive pyrimidinone benzimidazole skeleton was developed through nucleophilic substitution and Biginelli reaction starting from urea,ethyl 4-chloroacetoacetate and various *** target molecules exhibited strong antibacterial activities,especially pyrimidinone benzimidazole hybrid 9e possessed the strongest inhibitory effects on the growth of *** and *** with a lower MIC value of 1μg/mL than ***,compound 9e displayed strong antibiofilm capacity,low drug resistance and excellent biosafety toward human red blood *** research revealed that compound 9e could disrupt membrane integrity and cause leakage of cellular components such as proteins and nucleic ***,compound 9e could decrease lactate dehydrogenase activity,block cell metabolism and interact with DNA in an intercalation manner.
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