Iron (II) and Zinc (II) complexes of gemifloxacin mesylate: synthesis, characterization, serum binding profiling, and evaluation of antimicrobial activity

F. Aktar, Md. Jamal Hossain, Md. Zakir Sultan, M. Rashid
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Abstract

Gemifloxacin mesylate is a synthetic fluoroquinolone derived antimicrobial    agent. Two metal complexes of gemifloxacin mesylate were synthesized viz. gemifloxacin-Fe and gemifloxacin-Zn. The formed complexes were characterized by using TLC, TGA and FT-IR spectra analyses. The formed complexes were then evaluated for antimicrobial activity. The newly formed two complexes were assessed against nine bacterial and one fungal strain, where gemifloxacin (30 µg/disc) was used as a reference standard. The new complexes showed better activity than the standard reference drug against Klebsiella pneumoniae among nine bacterial strains. But two bacterial species, Acinetobacter lwoffii and Enterococcus faecium, and the fungal strain Candida albicans showed complete resistance to the newly synthesized complexes and the reference standard.  The drug protein interaction with the Bovine Serum Albumin (BSA) was also studied. The interaction mechanism was explored, suggesting that gemifloxacin and its Zn (II) complex interact with BSA via a static process while the Fe (II) complex interacts via a dynamic process and the lower Ksv value also indicated that drug -BSA complexes were formed in ground-state. J. Bangladesh Acad. Sci. 46(2); 203-211: December 2022       
甲磺酸吉氟沙星的铁(II)和锌(II)配合物:合成、表征、血清结合分析和抗菌活性评估
甲磺酸吉氟沙星是一种合成的氟喹诺酮类衍生抗菌剂。合成了两种甲磺酸吉米沙星金属配合物:吉米沙星铁和吉米沙星锌。通过TLC、TGA和FT-IR对所形成的配合物进行了表征。然后评估形成的配合物的抗菌活性。新形成的两个配合物对9种细菌和1种真菌菌株进行了评估,其中使用吉氟沙星(30µg/盘)作为参考标准。新复合物对肺炎克雷伯菌的活性优于标准参比药物。但伊沃菲不动杆菌和屎肠球菌两种细菌以及真菌菌株白色念珠菌对新合成的配合物和参比标准物表现出完全耐药。研究了药物蛋白与牛血清白蛋白(BSA)的相互作用。结果表明,吉氟沙星及其Zn (II)配合物与BSA的相互作用是静态的,而Fe (II)配合物与BSA的相互作用是动态的,Ksv值较低也表明药物与BSA的配合物是在基态下形成的。科学通报46(2);203-211: 2022年12月
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