Design, Synthesis, and Docking Studies of Arylhydrazone Compounds and Evaluation of Their Platelet Aggregation Inhibitory Effect and Cytotoxicity

In view of proven antiplatelet activity of hydrazone group containing compounds, two series of hydrazone derivatives were synthesized by coupling appropriate aldehydes with phenyl hydrazine and Isonicotinic acid in the presence of distilled water and a catalytic amount of glacial acetic acid. All synthesized compounds were screened for their antiplatelet activity against induced aggregation by adenosine diphosphate (ADP) and arachidonic acid (AA). The results indicate that compounds in arylhydrazone group had shown satisfactory activity. Among them, 1-(3-methoxybenzylidene)-2-phenylhydrazine (1c), 2-methoxy-4-(2-phenylhydrazono) methyl phenol (1g), and 2-((2-phenylhydrazono) methyl)-1H-pyrrole (1h) were found to be the most potent antiplatelet compounds with IC50 less than 39 μM. Furthermore, the cell toxicity assay, (MTT test) indicates their noncytotoxic in various cell lines. None of the synthesized N-isonicotinohydrazide derivatives in this study excreted sufficient antiplatelet activity.

Synthesis, Crystal Structure and Reversible Solid-State Crystal-to-Crystal Transformation of Three Isostructural Lead(II) Halide Coordination Polymers with different luminescence properties in bulk and nano scale

Novel three dimensional (3D) isostructural lead(II) halide coordination polymers [Pb(INO)X]n X= Cl (1) , Br (2), I (3); INO = isonicotinic acid n-oxide] have been synthesized via branched-tube method. The...

Investigation into the Protective Effects of Hypaconitine and Glycyrrhetinic Acid Against Chronic Heart Failure of the Rats

BackgroundThe present study aimed to determine the protective effects of hypaconitine (HA) and glycyrrhetinic acid (GA) against chronic heart failure (CHF) in the rats and to explore the underlying molecular mechanisms.Methods The CHF rat model was established by transverse-aortic constriction (TAC) operation. The total cholesterol (TCHO) and triglyceride (TG) levels were determined by ELISA assay. The protein expression of fibroblast growth factor 2 (FGF2), vascular endothelial growth factor A (VEGFA) and endothelial nitric oxide synthase (eNOS) in the rat ventricular tissues was determined by immunohistochemistry. The serum metabolites were determined by LC-MS/MS assay.ResultsHA + GA treatment significantly reduced the plasma levels of TCHO and TG in the CHF rats. The expression of FGF2 and VEGFA protein was up-regulated and the expression of eNOS protein was down-regulated in the ventricular tissues of CHF rats, which was significantly restored after HA + GA treatment. HA + GA treatment down-regulated serum isonicotinic acid, phosphatidylcholine, cardiolipin, estrogen glucuronide, and glycocholic acid, up-regulated serum sphingosine and deoxycholic acid in the CHF rats.ConclusionIn conclusion, HA +GA showed protective effects on CHF in the rats, and the HA + GA may exert protective effects by reducing lipid levels, up-regulating the expression of FGF2 and VEGFA proteins, attenuating eNOS protein expression, and modulating metabolic pathways. However, the molecular mechanisms underlying HA + GA-mediated effects still require further examination.

Pyrazine-2(1H)-thione

The title compound, C4H4N2S, was obtained by the reduction of 2-mercaptopyrazine (during its crystallization with 2-mercaptopyrazine and isonicotinic acid N-oxide in ethanol solution. It crystallizes in the monoclinic space group P21/m. In the crystal, the molecules are linked by N—H...N and C—H...S hydrogen bonds.

Synergistic Effect of Plant Defense Elicitors and Biocontrol Agents on Induction of Defense Enzymes in Pea against Downy Mildew

Background: Plant defense against the pathogens can be induced by using different defense inducers. Plants can be treated with elicitors for fast and more intense mobilization of defense responses which can enhance the resistance against biotic or abiotic stresses. Methods: The present study has been undertaken to evaluate the synergistic effect of different plant defense inducing chemical (Salicylic acid, Isonicotinic acid, Oxalic acid and Chitosan) and biological (Trichoderma harzianum and Pseudomonas fluorescens) elicitors. Enzyme activity was expressed as the increase in absorbance using spectrophotometer. Result: Among all the treatments the maximum PAL activity (35.58 mg/g of fresh weight) was found in case of oxalic acid but after 48 hrs its activity reduced drastically. Next to oxalic acid Pseudomonas fluorescens (31.38 mg/g of fresh weight), chitosan + Trichoderma harzianum (29.38 mg/g of fresh weight) and chitosan + Pseudomonas fluorescens (27.89 mg/g of fresh weight) showed the maximum enzyme activity. The PPO activity reached the highest at 96 hr after challenge inoculation in case of chitosan + Trichoderma harzianum (9.74 µmol/min/mg/protein) treated plants followed by Trichoderma harzianum (3.53 µmol/min/mg/protein) alone. the maximum PO activity (49.12 µmol/min/mg/protein) was found in case of chitosan + Pseudomonas fluorescens treated plants followed by chitosan (42.48 µmol/min/mg/protein) after 72 hrs. the maximum phenolics (27.53 mg/gm of fresh weight) was found in case of chitosan + Pseudomonas fluorescens after 48 hrs of treatment.