We report the synthesis, the antioxidant and the inhibitory activity (IC50) on metalloproteinases (MMPs) 3 and 13 of 2-benzo[d]isothiazolylimino-5-benzylidene-4-thiazolidinones. Their potential as protective agents in osteoarthritis (OA) was evaluated by biological assays on chondrocytes culture...
Large, diverse compound libraries are an essential requisite in target-based drug development. In this work, a robust microwave-assisted synthesis for the diastereoselective generation of 3-saccharinyl-trans-β-lactams is reported. The method is optimised for combinatorial library synthesis in w...
A series of 3,7-diaryl-6,7-dihydroisothiazolo [4,5-b]pyridin-5(4H)-ones 8 and 9 was synthesized by multicomponent condensation of 3-aryl-5-isothiazolecarboxylic acid esters 4a–f with aromatic (or thienyl) aldehydes 7 and Meldrum's acid in an acidic medium. The targeted compounds were evalu...
The flash vacuum pyrolysis (FVP) of 1H-benzotriazoles is an important and high-yielding source of cyanocyclopentadienes (cyclopentadienecarbonitriles). Early research on the pyrolysis of 1-acylbenzotriazoles only revealed formation of benzoxazoles, while the important formation of cyanocyclopent...
In this paper, we explore the copper/palladium-cocatalyzed cross-coupling reactions of 1-aryl-2-trimethylsilylethynes with aryl iodides, bromides, and chlorides as coupling partners, to furnish unsymmetrically disubstituted ethynes in moderate to excellent yields. Various aryl iodides were subje...
SummaryDuring cerebellar development, Sonic hedgehog (Shh) signaling drives the proliferation of granule cell precursors (GCPs). Aberrant activation of Shh signaling causes overproliferation of GCPs, leading to medulloblastoma. Although the Shh-binding protein Boc associates with the Shh recepto...
CuI-catalyzed coupling of 2-bromobenzylamines and α-amino acids and subsequent condensative cyclization (directly or mediated with DPPA) provides 1,4-benzodiazepin-3-ones in moderate yields. Using l-proline and l-valine as the starting materials enantiopure products are obtained although partia...
A series of 1,3,4-oxadiazole acetamide derivatives have been designed and synthesized, and their complexes with Eu(III) and Tb(III) were also prepared. The luminescence properties of the target complexes were investigated, and the results indicated that all target complexes showed the characteri...
Epidemiological studies have identified that the risk of cardiovascular events increases due to the decreased levels of high density lipoprotein-cholesterol and the elevated levels of low density lipoprotein-cholesterol. Herein, we report a novel series of N,N-3-phenyl-3-benzylaminopropionanilid...
Titanium oxo-clusters composed of {Ti4O2} and {Ti6O6} cores were synthesized from the direct reaction of Ti(OiBu)4 and 4-aminobenzoic acid (HABZ) in molar ratios 4:1, 2:1, and 1:1 at room temperature. The complex [Ti4O2(OiBu)10(ABZ)2] 0.7iBuOH 0.5C7H8 (1a) has been isolated from the 4:1 reaction...
The molecular structure, vibrational analysis and molecular docking analysis of the 3-Methyl-1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-aminobenzoate (MDDNAB) molecule have been carried out using FT-IR and FT-Raman spectroscopic techniques and DFT method. The equilibrium geometry, harmonic vibration...
Electroactive conducting copolymers of aniline (ANI) and ethyl 4-aminobenzoate (EAB) were prepared electrochemically. Cyclic voltammetric studies were carried out with different feed concentration of EAB on glassy carbon electrode surface. The voltammograms exhibited different behavior for diffe...
The synthesis, characterization and mesomorphism of new thermotropic imine prepared via condensation of biphenyl-4-carboxaldehyde with poly(1,4-butanediol)bis(4-aminobenzoate) was reported. The structure of imine was characterized by means FTIR, 1H, 13C NMR spectroscopy and elemental analysis; t...
The synthesis and study of trimethyl-, tributyl- and triphenyltin esters of the 3- and 4-aminobenzoic acids are reported. The triorganotin derivatives are characterized by elemental analyses, FT-IR and solution 1H and 13C NMR spectra. The structure of the trimethyltin 4-aminobenzoate is solved b...
The FT-IR and FT-Raman spectra of ethyl 4-aminobenzoate (EAB) in the solid phase were recorded. The fundamental vibrational wavenumbers, intensities of vibrational bands and the optimized geometrical parameters of the compound were evaluated using DFT (B3LYP) method with 6-311++G(d,p) basis set....
The synthesis and characterization of triazenes of the type 1-[2′-(methoxycarbonyl)phenyl]-3-[4′-X-phenyl]triazene [X = F (1), Cl (2), Br (3), I (4)] as precursors of triazenide ligands for the preparation of their complexes of formula [Ru{1-(2′-methoxycarbonylphenyl)-3-(4′-X-phenyl)triazeni...
Three polar Ni(II)-, Cu(II)- and Zn(II)-complexes (M-SSA) of salicylidene anthranilate sodium salt ligand were synthesized. The ligand (H2SSA) and its corresponding metal-complexes are characterized by alternative physico-chemical tools in which H2SSA acts as tridentate bi-basic chelating agent....
The ultrafast excited state dynamics of the sunscreen ingredient menthyl anthranilate (MenA) and its precursor methyl anthranilate (MA) were studied in vacuum (using time-resolved ion yield spectroscopy) and in solution (using transient electronic absorption spectroscopy). MenA and MA both show ...
A new trisubstituted derivative of phenylacetic acid methyl ester was isolated from a Pseudomonas syringae pv. papulans strain culture. It was characterized as the methyl ester of 2′,5′-dihydroxy-3′-nitrophenylacetic acid by spectral studies of the metabolite and the corresponding diacetylder...
The ethanol content and esterase and alcohol acyltransferase activities are the limiting factors in the synthesis of ethyl esters in Camembert-type cheeses. This study aimed to investigate the effects of alcohol, esterase and alcohol acyltransferase activities on ethyl ester formation in Camembe...
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