Kassab Refaie M, Zaki Magdi E A, Al-Hussain Sami A, Abdelmonsef Aboubakr H, Muhammad Zeinab A
Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt.
Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623, Saudi Arabia.
ACS Omega. 2024 Jan 9;9(3):3349-3362. doi: 10.1021/acsomega.3c06348. eCollection 2024 Jan 23.
: Design and synthesis of antimicrobial prototypes that are capable of eradicating bacterial biofilm formation that is responsible for many health challenges particularly with antibiotic-resistant bacterial species. : The utility of 1,3-diarylenones, chalcones, - and - as building blocks to construct the corresponding bis-pyrazoline derivatives and . Screening the antibacterial behavior of the novel bis-pyrazoline derivatives against methicillin-sensitive (MSSA), methicillin-resistant (MRSA), and vancomycin-resistant (VRSA) bacterial strains was investigated. : Chalcones were used as building scaffolds to construct two series of di- and trisubstituted bis-pyrazoline derivatives. Numerous novel bis-compounds displayed decent bacterial biofilm suppression. : Two regioisomeric series of bis-chalcones were designed and constructed, and their structural diversity was manipulated to access the intrinsically bioactive, pyrazoline ring. The newly synthesized bis-pyrazoline derivatives presented decent antibacterial behavior against multiple drug-resistant bacterial strands (MSSA, MRSA, and VRSA).
设计和合成能够消除细菌生物膜形成的抗菌原型，细菌生物膜形成是许多健康挑战的原因，尤其是对抗生素耐药的细菌种类。：以1,3 - 二芳基烯酮、查耳酮等为构建单元来构建相应的双吡唑啉衍生物和。研究了新型双吡唑啉衍生物对甲氧西林敏感金黄色葡萄球菌（MSSA）、耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素金黄色葡萄球菌（VRSA）菌株的抗菌行为。：查耳酮用作构建支架来构建两个系列的二取代和三取代双吡唑啉衍生物。许多新型双化合物表现出良好的细菌生物膜抑制作用。：设计并构建了两个区域异构体系列的双查耳酮，并对其结构多样性进行调控以获得具有内在生物活性的吡唑啉环。新合成的双吡唑啉衍生物对多重耐药细菌株（MSSA、MRSA和VRSA）表现出良好的抗菌行为。
