Baaiu Basma Saad, Saleh Nashwa M, Alshref Aldirsi Abdulrahman Faraj, Abdel-Aziem Anhar
Department of Chemistry, Faculty of Science, Benghazi University, Benghazi, Libya.
Department of Chemistry, Faculty of Science (Girls), Al-Azhar University, Nasr City, Cairo, Egypt.
Future Med Chem. 2025 Jan;17(1):9-18. doi: 10.1080/17568919.2024.2437974. Epub 2024 Dec 12.
Developing new antimicrobial agents in response to the urgent challenge of antimicrobial resistance.
Synthesis of the targeted coumarins, elucidation of their structures using spectroscopic tools, and investigation of their antimicrobial activity.
Coumarin-pyrazole with CF in the 3-position of the pyrazole ring displayed the lowest minimum inhibitory concentrations (MICs) and the minimum bactericidal concentrations (MBCs) with values of 1.95 and 15.6 µg/ml, respectively, against . In addition, it exhibited the best inhibitory activity against (MIC = 3.91 µg/ml) compared to the rest of the derivatives (7.81-62.5 µg/ml). Surprisingly, coumarin with the S-CH group had higher ability to inhibit the strain with an MIC value of , which is twice that of penicillin G (). At the same time, compounds , , , , and penicillin G showed similar activity with an MIC value of against . Also, the lowest MIC value (3.91 µg/ml) was obtained for S-CH derivative against . Coumarins and 1,3,4-thiadiazine derivative recorded the lowest MBC (15.6 µg/ml) against .
Finally, it can be concluded that some designed coumarins have a high potential to act as potent antimicrobial agents. Some of them displayed higher efficacy than or equal to the reference drug.
应对抗菌药物耐药性这一紧迫挑战,研发新型抗菌剂。
合成目标香豆素,使用光谱工具阐明其结构,并研究其抗菌活性。
吡唑环3位带有CF的香豆素 - 吡唑对[具体细菌名称缺失]的最低抑菌浓度(MIC)和最低杀菌浓度(MBC)分别为1.95和15.6μg/ml,为最低值。此外,与其他衍生物(7.81 - 62.5μg/ml)相比,它对[具体细菌名称缺失]表现出最佳抑制活性(MIC = 3.91μg/ml)。令人惊讶的是,带有S - CH基团的香豆素抑制[具体细菌名称缺失]菌株的能力更强,MIC值为[具体数值缺失],是青霉素G([具体数值缺失])的两倍。同时,化合物[具体化合物编号缺失]和青霉素G对[具体细菌名称缺失]的MIC值相似,均为[具体数值缺失]。此外,S - CH衍生物对[具体细菌名称缺失]的MIC值最低(3.91μg/ml)。香豆素[具体化合物编号缺失]和1,3,4 - 噻二嗪衍生物对[具体细菌名称缺失]的MBC最低(15.6μg/ml)。
最后,可以得出结论,一些设计的香豆素具有作为强效抗菌剂的高潜力。其中一些表现出比参考药物更高或与之相当的疗效。