Synthesis, structural characterization, and antimicrobial evaluation of new mononuclear mixed ligand complexes based on furfural-type imine ligand, and 2,2'-bipyridine.

The present investigation goal was to investigate the chemistry of four new mononuclear mixed ligand Fe(III), Co(II), Cu(II), and Cd(II) complexes constructed from furfural-type imine ligand (L), and the co ligand 2,2'-bipyridine in addition to assessing their antimicrobial activity against some bacterial, and fungi strains. The structure of the complexes was interpreted by different spectroscopic techniques such as MS, IR, 1H NMR, UV-Vis, elemental analysis, TG-DTG, conductivity, and magnetic susceptibility measurements. The correlation of all results revealed that ligand (L) acts as a neutral ONNO tetradentate whereas the co ligand acts as a neutral NN bidentate. The coordination of the ligands with the metal ions in a molar ratio of 1:1:1 leads to formation of an octahedral geometry around the metal ions. The octahedral geometry has been validated and optimized by DFT analysis. Conductivity data showed the electrolytic nature of all complexes. The thermal stability of all complexes was deduced in addition to evaluating some thermodynamic, and kinetic parameters using Coats-Redfern method. Furthermore, all complexes in comparison to their parent ligands were tested for their biological potency against some pathogenic bacterial, and fungi strains using the paper disk diffusion method. [CdL(bpy)](NO3)2 complex revealed the highest antimicrobial activity.

Analysis of [11C]methyl-candesartan kinetics in the rat kidney for the assessment of angiotensin II type 1 receptor density in vivo with PET.

INTRODUCTION: Angiotensin II type 1 (AT(1)) receptors play a key role in the regulation of renal and cardiovascular functions and have been implicated in the pathogenesis of many diseases. The aim of this study was to assess binding of the novel radioligand [(11)C]methyl-candesartan to AT(1) receptors in the rat kidney in vivo with PET. METHODS: Dynamic PET images were acquired for 60 min at baseline, with coinjection of candesartan (5 mg/kg), and after injection of PD123,319 (5 mg/kg). Volumes of distribution (R(C)∙V(T)) were estimated with a two-compartment model, by Logan analysis, and by taking the tissue-to-plasma activity ratio at 50-60 min post-injection. RESULTS: The two-compartment model did not describe the kinetics at baseline adequately and the baseline scans were too short to obtain accurate estimates of R(C)∙V(T) with the Logan approach. Based on the tissue-to-plasma ratios, roughly one-third of V(T) at baseline could be attributed to AT(1) receptor binding. There were no indications of AT(2) receptor binding in the rat kidney. CONCLUSION: It may be possible to detect changes in AT(1) receptor density in the rat kidney in vivo with [(11)C]methyl-candesartan and PET. Imaging AT(1) receptors with PET may provide valuable information on the role of these receptors in the pathogenesis of diseases such as hypertension, diabetic nephropathy, ventricular remodeling, and heart failure.