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关于供体 tethered 铜(II)和钒(V)配合物作为有效的抗结核和抗真菌剂及其与光谱法研究的人血清白蛋白(HSA)相互作用

ON donor tethered copper (II) and vanadium (V) complexes as efficacious anti-TB and anti-fungal agents with spectroscopic approached HSA interactions.

作者信息

Sinha Anamika, Chaudhary Riya, Reddy Dinesh S, Kongot Manasa, Kurjogi Mahantesh M, Kumar Amit

机构信息

Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Bengaluru, 562112, Karnataka, India.

Multi-Disciplinary Research Unit, Karnataka Institute of Medical Sciences, Hubli, India.

出版信息

Heliyon. 2022 Aug 11;8(8):e10125. doi: 10.1016/j.heliyon.2022.e10125. eCollection 2022 Aug.

Abstract

Antimicrobial drug resistance poses a significant threat worldwide, hence triggering an urgent situation for developing feasible drugs. 3D-transition metal coordination complexes being multifaceted, offer tremendous potency as drug candidates. However, there are fewer reports on non-toxic and safe transition metal complexes; therefore, we hereby attempted to develop novel copper and vanadium-based therapeutic agents. We have synthesised six metal complexes , [VO(Quibal-INH)] , [Cu(Quibal-INH)] , [VO(Quibal-INH) (cat)] , [Cu(Quibal-INH) (cat)] , [VO(Quibal-INH) (bha)] and [Cu(Quibal-INH) (bha)] . Quibal-INH is an ON bidentate donor ligand synthesized from Schiff base reaction between 4-(2-(7-chloroquinolin-3-yl)vinyl)benzaldehyde (Quibal) and Isoniazid (INH). The synthesized compounds were characterized using analytical techniques involving ATR-IR, UV-Vis, EPR, H NMR, C NMR, and V NMR. Ligand and compound exhibited moderate growth inhibitory activity towards and fungal species. Compound has been identified as active against the above fungal species with no toxicity and hemolysis activity on the healthy cells. Compound exhibited significant activity against the strain. Further, compounds , and exhibited excellent free radical scavenging activity. All the developed compounds were found to exhibit stability over a wide range of pH conditions. The complexes were additionally studied for their interaction with human serum albumin (HSA) with the UV-vis spectroscopic technique.

摘要

抗菌药物耐药性在全球构成重大威胁,因此引发了开发可行药物的紧迫形势。三维过渡金属配位络合物具有多方面特性,作为候选药物具有巨大潜力。然而,关于无毒且安全的过渡金属络合物的报道较少;因此,我们在此尝试开发新型铜基和钒基治疗剂。我们合成了六种金属络合物,[VO(Quibal-INH)]、[Cu(Quibal-INH)]、[VO(Quibal-INH)(cat)]、[Cu(Quibal-INH)(cat)]、[VO(Quibal-INH)(bha)]和[Cu(Quibal-INH)(bha)]。Quibal-INH是一种ON双齿供体配体,由4-(2-(7-氯喹啉-3-基)乙烯基)苯甲醛(Quibal)和异烟肼(INH)之间的席夫碱反应合成。使用包括ATR-IR、UV-Vis、EPR、1H NMR、13C NMR和51V NMR在内的分析技术对合成的化合物进行了表征。配体和化合物对细菌和真菌物种表现出中等的生长抑制活性。化合物已被确定对上述真菌物种具有活性,对健康细胞无毒性和溶血活性。化合物对该菌株表现出显著活性。此外,化合物、和表现出优异的自由基清除活性。发现所有开发的化合物在很宽的pH条件范围内都具有稳定性。还使用紫外可见光谱技术研究了这些络合物与人血清白蛋白(HSA)的相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5888/9403362/434a4350423d/ga1.jpg

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