Condensation of 4-benzoyl-1,2-phenylenediamine with sodium pyruvate in acetic acid furnished two products which were identified as 6-benzoyl and 7-benzoyl-3-methyl-2(1H)quinoxalinones (1a,b). Fusion of 1a with aromatic aldehydes furnished the styryl derivatives 2a-c. Alkylation of 1a,b with dimethyl sulphate or ethyl chloroacetate produced the N-alkyl derivatives 3a,b and 4a,b. Hydrazinolysis of the ester derivative 4a with hydrazine hydrate afforded the hydrazide derivative 5 which underwent condensation with aldehydes to give the corresponding hydrazone derivatives 6a,b. In addition, chlorination of 1a with thionyl chloride afforded the 2-chloro derivative 7 which was subjected to reaction with sodium azide and n-butylamine to yield the corresponding tetrazolo (8) and n-butylamino (9) derivatives, respectively. The structures of the compounds prepared were confirmed by analytical and spectral data. Also, some of the synthesized compounds were screened for antimicrobial activity.
Stress is any condition that impairs the balance of the organism physiologically or psychologically. The response to stress involves several neurohormonal consequences. Glutamate is the primary excitatory neurotransmitter in the central nervous system, and its release is increased by stress that predisposes to excitotoxicity in the brain. Memantine is an uncompetitive N-methyl D-aspartate glutamatergic receptors antagonist and has shown beneficial effect on cognitive function especially in Alzheimer's disease. The aim of the work was to investigate memantine effect on memory and behavior in animal models of acute and repeated restraint stress with the evaluation of serum markers of stress and the expression of hippocampal markers of synaptic plasticity. Forty-two male rats were divided into seven groups (six rats/group): control, acute restraint stress, acute restraint stress with Memantine, repeated restraint stress, repeated restraint stress with Memantine and Memantine groups (two subgroups as positive control). Spatial working memory and behavior were assessed by performance in Y-maze. We evaluated serum cortisol, tumor necrotic factor, interleukin-6 and hippocampal expression of brain-derived neurotrophic factor, synaptophysin and calcium-/calmodulin-dependent protein kinase II. Our results revealed that Memantine improved spatial working memory in repeated stress, decreased serum level of stress markers and modified the hippocampal synaptic plasticity markers in both patterns of stress exposure; in ARS, Memantine upregulated the expression of synaptophysin and brain-derived neurotrophic factor and downregulated the expression of calcium-/calmodulin-dependent protein kinase II, and in repeated restraint stress, it upregulated the expression of synaptophysin and downregulated calcium-/calmodulin-dependent protein kinase II expression.
Photoinduced graft copolymerization of acrylamide (AM) onto two types of acrylonitrile-butadiene-styrene (ABS) copolymers was extensively investigated in homogeneous media. The grafting process was conducted in chloroform in presence of 4-acetyldiphenyl(4-AD). Ultraviolet (UV) irradiation was used in the range of 310 to 460 nm. The UV spectrum of 4-AD has X , , , at 285 nm and shows n -T* transitions. The grafting parameters, such as weight conversion, grafting percentage, and grafting efficiency, were determined as a function of the irradiation time and the concentrations of monomer, initiator, and substrate. A reverse effect
The reaction of cyanoacetanilide derivative 1 with some electrophiles was investigated. Treatment of compound 1 with 2-(2-oxoindol-3-ylidene)malononitrile (2a) under reflux in ethanol in the presence of piperidine afforded the spiro[indoline-3,4′-pyridine] derivative 3. Under similar conditions, condensation of compound 1 with the analog 2b yielded a spiroindole 4. Chromeno[3,4-c]pyridine derivative 6 was obtained by cyclization of chromene derivative 5 with ethyl cyanoacetate. In a similar manner, condensation of compound 5 with cylcohexanone under reflux in ethanol in the presence of sodium acetate furnished chromeno[3,4-c]quinoline derivative 7. Compound 1 was condensed with 2-hydroxy-1-naphthaldehyde to yield the benzo[f]chromeno derivative 8. Refluxing of benzochromene derivative 8 with ethyl cyanoacetate in ethanol in the presence of catalytic amount of piperidine produced benzo[f]chromeno[3,4-c]pyridine derivative 9. The structures of the newly synthesized compounds were confirmed on the basis of analytical and spectral data.
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