Abstract Pancreatic lipase (PL) inhibitors have received considerable attention by several researchers because of its ability to hydrolyse the triglycerides in small intestine. This study reports (i) synthesize new pyrazole derivatives binding amino acid and Dicyclohexylurea (DCU), (ii) their pharmaceutical potentials‐ via enzyme inhibitory activity towards PL antioxidant activities (using complementary methods including FCR, FRAP ORAC), (iii) possible interactions between compounds through...

4-Acyl-pyrazole-3-carboxylic acids (1) were synthesized via the reaction of 4-acyl-2,3-furandiones (F) with hydrazone (1-benzylidene-2-(2,5-dimethyl-phenyl)-hydrazine) by heating under solid phase and their acid chlorides (2) obtained. Then these derivatives easily converted into corresponding such as ester, amide, ureide, pyrazolo-pyridazine, etc. Totally 62 new compounds synthesized. The structures determined spectroscopic methods in vitro antibacterial activity newly carried out against...

Background: Glioblastoma Multiforme (GBM), a highly aggressive and prevalent brain cancer with higher incidence in males, has limited treatment success due to drug resistance, inadequate targeting penetration of cells, an incomplete understanding its molecular pathways. GBM is options. This study investigates the anticancer potential synthesized pyrazole compounds against cells. Methods: A series derivatives were tested for their efficacy using MTT assays. Molecular docking studies conducted...

Abstract γ‐aminobutyric acid (GABA) is the main neuroinhibitory transmitter and a non‐proteinogenic amino in brain. When brain concentration of GABA diminishes below threshold level, it can cause excess neuronal excitation lead to convulsions. γ‐Aminobutyric aminotransferase (GABA‐AT) an enzyme that catalyzes conversion succinic semialdehyde shunt pathway responsible for breaking down By inhibiting GABA‐AT activity, may be possible increase levels reduce likelihood seizures. Herein,...

A series of tetrasubstituted pyrazole-3-carboxamides (3a?c) and pyrazole- 3-carbonyl thioureides (6a?c) were synthesized their structures characterized by IR, NMR elemental analysis. The antibacterial potential against specific Gram-positive Gram-negative strains the antifungal activities all novel compounds investigated. Structure?activity relationships (SAR) studies some theoretical parameters (ClogP, CMR, PSA ESP) performed on these two pyrazole derivatives. Pyrazole-3-carboxylate ester 2...

Pyrazole-3,4-dicarboxylic acid 2 was synthesized via the hydrolysis of pyrazole-3-carboxylic 1 and subsequently heated with thionyl chloride to give novel pyrazole-3,4-dicarbonyl dichloride 3, which easily converted into oligo-pyrazole 4 upon its reaction p-phenylene-diamine. These newly compounds were characterized by 1H-NMR, 13C-NMR, FT-IR spectroscopy, gel permission chromatography (GPC). Three thin films prepared using these respective values thickness: 20, 21, 24 μm. The optical...

Abstract magnified image 1,5‐Diphenyl‐1 H ‐pyrazole‐3,4‐dicarboxylic acid‐4‐ethyl ester 2 , obtained from the 4‐ethoxycarbonyl‐5‐phenyl‐2,3‐furandione 1 and N ‐benzylidene‐ ′‐phenyl hydrazine, was converted via reactions of its acid chloride 3 with various alcohols or N‐nucleophiles into corresponding 5 amide derivatives 6 respectively. In addition, decarboxylated to give ethyl 1,5‐diphenylpyrazole‐4‐carboxylate 4 . Nitrile 7 derivative also by dehydration 6a in a mixture SOCl DMF. While...

Abstract magnified image Cycloaddition of acetylbenzoyl ketene generated in situ as an intermediate during one‐step reaction between excess benzoylacetone and oxalylchloride to C=C double bond cyclic enol form gave 3‐acetyl‐5‐benzoyl‐6‐methyl‐2‐phenyl‐4(4 H )‐pyrone 1a . Condensation reactions together with 3,5‐dibenzoyl‐2,6‐diphenyl‐4(4 1b 3‐benzoyl‐5‐ethoxycarbonyl‐2,6‐diphenyl‐4(4 1c two‐fold primary amines provided a series 3‐benzoyl‐1‐alkyl‐5‐(1‐alkylimino‐ethyl)‐6‐phenyl‐2‐methyl‐4(1...

Some new pyrazole‐, chromone‐, or oxadiazole‐substituted 1H‐pyrazoles were obtained via 2,3‐furandiones. Also, we have presented their plausible mechanisms based on rearrangement; one of these rearrangements is Baker–Venkataraman.

3-Acetyl-5-benzoyl-6-methyl-2-phenyl-4H-pyran-4-one has been subjected to condensation with a series of primary amines (ethylamine - octylamine) clarify the proposed mechanism in our previous study. The reactions shorter butylamine) yielded unsymmetric pyridinone products, whereas other (pentylamine symmetrical pyridinones. starting material and products as well intermediates have theoretical analysis by quantum chemical calculations at B3LYP/6-31G(d,p) level, which provided supporting data...

In this study, a series of asymmetric aryl 1,3-dicarbonyl compounds were synthesized and their enol forms observed via experimental data theoretical calculations. According to the 1H- 13C-NMR results, all investigated found as single form in CDCl3 solution. Moreover, HMBC spectra applied identify correlations between certain protons carbon atoms considered. The dihedral angles that have units on both sides calculated by DFT understand reason for forms. Small caused longer conjugation,...

Abstract For see ChemInform in Full Text.

The chiral substituted pyrazole-3-carboxamides (4a-c), pyrazole-3-carboxylates (5a-c), pyrazole-3-thioureides (7a-c) and pyrazole-3,4-dicarboxamides (10a-c) were prepared via the pyrazolo-3-chlorocarbonyl 2, pyrazolo-3,4-dicarboxy methyl ester 3 with pyrazole-3-isothiocyanate 6 different (R)-chiral amino alcohols. All of synthesized compounds binding a pyrazole skeleton investigated as organocatalysts for asymmetric aldol reactions between nitromethane p-nitrobenzaldehyde in presence CuCl....

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 200 leading journals. To access Abstract, please click on HTML or PDF.