Design, synthesis and characterization of novel 2-(2,4-disubstituted-thiazole-5-yl)-3-aryl-3H-quinazoline-4-one derivatives as inhibitors of NF-κB and AP-1 mediated transcription activation and as potential anti-inflammatory agents

Synthesis, in vitro anticancer screening and radiosensitizing evaluation of some new 4-[3-(substituted)thioureido]-N-(quinoxalin-2-yl)-benzenesulfonamide derivatives

“…-A mixture of 2 (0.342 g, 0.001 mol) and 2-amino-5-bromopyridine (0.173 g, 0.001 mol) in DMF (20 mL), containing 3 drops of TEA, was refluxed for 5 h. The solid obtained was precipitated while hot and filtered to give compound 5. (6). -The mixture of 2 (0.342 g, 0.01 mol) and p-bromoaniline (0.171 g, 0.001 mol) in dioxane (20 mL), with 3 drops of TEA, was refluxed for 1 h, the solid obtained was precipitated when cold and filtered to give compound 6.…”

“…All compounds were within ±0.4 % of theoretical values. The IR spectra (KBr) were measured on a Shimadzu IR 110 Spectrophotometer (Shimadzu, Japan), 1 H NMR and 13 C NMR spectra were obtained with a Bruker proton NMR-Avance 300 instrument (300 MHz) (Bruker, Germany), in DMSO-d 6 as a solvent, using tetramethylsilane (TMS) as internal standard. Mass spectra were run using an HP Model MS-5988 (Hewlett Packard, USA).…”

Synthesis and spectral characterization of some heterocyclic nitrogen compounds

“…Pyrimidines [7] encourage the authors to gather these moieties hoping to produce valuable new compounds of expected antibacterial and antifungal activity. We report here the synthesis of novel quinazolin-2,4-dione derivatives starting from (2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-acetic acid hydrazide (3). All the synthesized compounds have been supported by their spectral data.…”

“…Scheme 2 outlines the synthetic pathway used to obtain 3-(5-thioxo- [1,3,4]oxadiazolidin-2-ylidenemethyl)-1H-quinazoline-2,4-dione (4) which prepared by treatment of compound 3 with with carbon disulphide in pyridine under reflux for 9 hrs. as given mechanism in Scheme 4.…”

“…As an important class of electron-rich N-containing heterocycles, pyrimidines are widely present in biologically active compounds and have also versatile synthetic applications. Many derivatives of pyrimidines showed antifungal [1], antibacterial [2], anti-inflammatory [3] anticonvulsant [4][5][6]. Pyrimidines [7] encourage the authors to gather these moieties hoping to produce valuable new compounds of expected antibacterial and antifungal activity.…”