Faidallah Hassan M, Girgis Adel S, Tiwari Anand D, Honkanadavar Hitesh H, Thomas Sean J, Samir Ahmed, Kalmouch Atef, Alamry Khalid A, Khan Khalid A, Ibrahim Tarek S, Al-Mahmoudy Amany M M, Asiri Abdullah M, Panda Siva S
Department of Chemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
Pesticide Chemistry Department, National Research Centre, Dokki, Giza 12622, Egypt.
Eur J Med Chem. 2018 Jan 1;143:1524-1534. doi: 10.1016/j.ejmech.2017.10.042. Epub 2017 Oct 16.
A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10-15, 17-19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17-19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1-3. 2D-QSAR modeling supports the observed biological properties.
通过微波辅助点击化学技术合成了一组含1,2,3-三唑的喹诺酮抗生素缀合物10 - 15、17 - 19。一些芳基取代的缀合物17 - 19对测试的革兰氏阳性菌（金黄色葡萄球菌和化脓性链球菌）和革兰氏阴性菌（伤寒沙门氏菌）显示出有前景的抗菌特性，其效力高于母体抗生素1 - 3。二维定量构效关系建模支持所观察到的生物学特性。
