Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, United States.
Department of Pesticide Chemistry, National Research Centre, Dokki, Giza 12622, Egypt.
Med Chem. 2021;17(1):71-84. doi: 10.2174/1573406415666190904143852.
Bacterial infections are considered as one of the major global health threats, so it is very essential to design and develop new antibacterial agents to overcome the drawbacks of existing antibacterial agents.
The aim of this work is to synthesize a series of new fluoroquinolone-3-carboxamide amino acid conjugates by molecular hybridization. We utilized benzotriazole chemistry to synthesize the desired hybrid conjugates.
All the conjugates were synthesized in good yields, characterized, evaluated for their antibacterial activity. The compounds were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Synthesized conjugates were tested for activity against medically relevant pathogens; Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27856) Staphylococcus aureus (ATCC 25923) and Enterococcus faecalis (ATCC 19433).
The observed antibacterial experimental data indicates the selectivity of our synthesized conjugates against E.Coli. The protecting group on amino acids decreases the antibacterial activity. The synthesized conjugates are non-toxic to the normal cell lines. The experimental data were supported by computational studies.
细菌感染被认为是全球主要健康威胁之一，因此设计和开发新型抗菌剂以克服现有抗菌剂的缺点非常重要。
本工作旨在通过分子杂交合成一系列新型氟喹诺酮-3-羧酰胺氨基酸缀合物。我们利用苯并三唑化学合成了所需的杂合缀合物。
所有缀合物均以良好的产率合成、表征，并对其抗菌活性进行了评价。化合物的抗菌活性通过改编自临床和实验室标准协会的方法进行筛选。合成的缀合物针对与医学相关的病原体进行了活性测试;大肠杆菌(ATCC 25922)、铜绿假单胞菌(ATCC 27856)、金黄色葡萄球菌(ATCC 25923)和粪肠球菌(ATCC 19433)。
观察到的抗菌实验数据表明，我们合成的缀合物对大肠杆菌具有选择性。氨基酸上的保护基降低了抗菌活性。合成的缀合物对正常细胞系无毒性。实验数据得到了计算研究的支持。
