On treatment of copper(II) acetate with aryl hydrazone ligands, four new solid derivatives of copper(II) were produced in appreciable yields. Various characterization techniques including infrared, UV–visible, NMR, electron paramagnetic resonance and mass spectroscopies, elemental analysis, scanning electron microscopy, powder X‐ray diffraction and thermogravimetric analysis revealed a tetra‐coordination in all the mononuclear crystalline complexes with high thermal stability. Further, significant interaction of these novel complexes with calf thymus DNA via intercalative mode of binding was revealed by electronic absorption spectroscopy. The chemical nuclease activity of the complexes on pBR322 DNA was investigated in the presence and absence of oxidizing agent (H2O2). A potent nuclease activity was observed only in the presence of H2O2. Further, antibacterial and antifungal studies of the new ligands and complexes revealed that the latter possessed comparatively better activity.
A new series of Pyrazolo [3,4-d]pyrimidine containing amide derivatives (8 a-l) were designed, synthesized, and evaluated for their in vitro α-amylase inhibitory activity. The IC 50 values of the target compounds ranged from 1.60 � 0.48 to 2.04 � 1.20 μM as compared to the standard acarbose 1.73 � 0.05 μM. All the Pyrazolo[3,4-d]pyrimidine amide derivatives displayed good inhibitory activities, while seven analogs (8 d, 8 f, 8 g, 8 h, 8 i, 8 j and 8 k) exhibited more or less equipotent activity with IC 50 values 1.77 � 2.84, 1.65 � 0.45, 1.66 � 2.24, 1.73 � 0.37, 1.60 � 0.48, 1.75 � 0.36 and 1.64 � 0.03 μM respectively. Further, the most potent α-amylase inhibitors 8 d and 8 k were also screened for their in vivo antidiabetic activity against alloxan induced diabetic rat model at the dose of 25 and 50 mg/kg. Oral administration of these tested compounds significantly reduced the fasting blood glucose levels in dose dependent manner. The hypoglycemic effects of these compounds were more evident at 3 h and 5 h after administration of tested compounds which was similar to the effect displayed by the positive control. In addition, the binding energies calculated from the docking studies with the α-amylase enzyme (PDB ID: 1HNY) and biological activities indicate that the compounds containing nitro moiety on the phenyl group contributed significantly towards the antidiabetic activity.[a] Dr.
The reactions of the heteroleptic zirconium diisopropoxide bis(acetylacetonate) in benzene solution with two equivalents of oximes, alkoxyalkanols, triphenylsilanol and trimethylsilyl acetate yield products with the formula [{MeC(O)CHC(O)Me}2ZrL2] with L = —ONC(Me)C5H4N‐2, —ONC(Me)C4H3O‐2, —OCH2CH2OR (R = Me, Et, Bun; py = pyridine, fu = furan), —OSiPh3 and —OSiMe3. Most of these derivatives are solids, but the [(acac)2Zr(OSiMe3)2] is a viscous oil. They could be purified either by recrystallization or by vacuum distillation; all of these are monomeric in boiling benzene. Their elemental analyses, molecular weight measurements and IR as well as NMR spectra were measured. The oximato complex [(acac)2Zr{ONC(Me)py‐2}2] has been shown by single crystal X‐ray crystallography to be monoclinic and mononuclear in the solid state, where zirconium has the coordination number 8; all the ligands are situated in cis‐ position and the oximato ligand binds via N and O in a dihapto (η2‐N, O) manner.
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