Synthesis and Antioxidant Activity of New Thiazole Analogues Possessing Urea,Thiourea, and Selenourea Functionality

A new series of urea, thiourea, and selenourea derivatives with thiazole moieties were synthesized by the nucleophilic addition reaction of (2-amino-4-(3-chlorophenyl)thiazol-5-yl)(2-chlorophenyl)methanone with various substituted isocyanates/ isothiocyanates/isoselenocynates in acetone having a catalytic amount of sodium hydroxide at room temperature with good yields. All the synthesized compounds were fully characterized by spectroscopic data and screened for their in vitro antioxidant activity using 1,1-diphenylpicrylhydrazyl (DPPH), nitric oxide (NO), and hydrogen peroxide (H₂O₂) radical scavenging methods. A preliminary study of the structure–activity relationship revealed that the compounds containing selenourea functionality along with halogen group have exhibited potent activity (IC₅₀ ≤ 0.0309 µmol/mL) compared to the standards (IC₅₀ ≤ 0.0814 µmol/mL). Thus the title compounds are a new class of potent antioxidant agents and worthy of further investigation.     

Inhibition of LPS-induced no production in RAW264.7 cell lines: synthesis and molecular modeling of α-ketophosphonates of febuxostat

In an effort to develop novel anti-inflammatory agents, we synthesized phosphorylated derivatives of febuxostat using various phosphates/phosphonites by Michaelis-Arbuzov reaction. Their inhibitory activity on nitric oxide (NO) production, reactive oxygen species (ROS) production and cytotoxicity were evaluated using lipopolysaccharide (LPS) activated macrophages RAW264.7 assay, flow-cytometry analysis and MTT method respectively. Some of these compounds showed potent inhibition of NO and ROS production without obvious cytotoxicity. Furthermore, docking simulations were performed to positional compounds 3g, 3h, 3i and 3j into the COX-2 active site to determine the probable binding model. Physicochemical parameters revealed that most of the compounds possessed drug-like properties.     

Meson spectroscopy with confined one gluon exchange potential

Confined gluons-exchange among relativistically confined quarks is used to calculate the ground state masses and the radially excited states of pseudo scalar and vector mesons. A good agreement is obtained with the experimental masses. The limitation of the perturbative treatment of estimating theN−Δ andπ−ρ splitting using one-gluon-exchange potential is pointed out.     

Synthesis,Molecular Docking,Analgesic, and Anti-Inflammatory Activities of New 1,2,4-Oxadiazolo-Sulfonamides

Russian Journal of General Chemistry - In the present study novel 1,2,4-oxadiazolo sulfonamides 3a–3o are synthesized by an efficient method based on the reaction of 1,2,4-oxadiazole amines...     

Mild and Efficient Tf2O-Mediated Synthesis of 3-Amino-1-benzofurans

Russian Journal of Organic Chemistry - A mild and efficient procedure has been developed for the synthesis of 3-amino-1-benzofurans by intramolecular cyclization of the corresponding...     

Heavy quarkonia spectra and their decays in a relativistic quark model

Using the phenomenological relativistic harmonic model (RHM) for quarks, we have obtained the masses of S wave charmonium and bottomonium states. The full Hamiltonian used in the investigation has Lorentz scalar plus vector confinement potential, along with the confined one gluon exchange potential (COGEP). A good agreement with the experimental masses for the ground and the radially excited states is obtained both for the triplet and singlet S wave mesons. The decay properties of the ground state charmonium and bottomonium are investigated.