Synthesis and Anticonvulsant Activity of Novel 2- and 3-14-(Trisubstituted Pyridy1)-phenylaminol- and 2-[3- and 4-(Trisubstituted Pyridy1)-phenoxylquinoxaline Derivatives

A series of novel quinoxaline derivatives linked to a pyridine moiety through phenylamino or phenoxy residue was synthesized and evaluated as candidate anticonvulsants. The synthesis was achieved through reaction of 2,3-dichloroquinoxaline (1) with an equimolar amount of 4-aminoacetophenone to give compound 2 which is considered as an important synthon for the construction of a pyridine ring via several synthetic routs. Some compounds were synthesized through formation of the intermediate α,β-unsaturated compounds which, in turn, were allowed to react with malononitrile to give the corresponding alkoxypyridines (8-17). Compounds 18-21 were synthesized by a one-pot simple reaction between 2, the appropriate aldehyde, and malononitrile in sodium alkoxide solution. Moreover, they can be synthesized through reaction of compound 2 and arylidenemalononitrile in sodium alkoxide. The phenoxy analogues were prepared by reaction of 1 with 4-hydroxyacetophenone or 3-hydroxybenzaldehyde to give 22 and 27, respectively. These compounds, in turn, were allowed to react with malononitrile and the proper carbonyl compound in presence of sodium alkoxide in a one-pot reaction technique to give the target compounds. Biological evaluation of the prepared compounds showed that some of them are potent anticonvulsant agents. The detailed synthesis, spectroscopic and biological data are reported.</jats:p

Synthesis and Anticonvulsant Activity of Novel 2- and 3-14-(Trisubstituted Pyridy1)-phenylaminol- and 2-[3- and 4-(Trisubstituted Pyridy1)-phenoxylquinoxaline Derivatives

A series of novel quinoxaline derivatives linked to a pyridine moiety through phenylamino or phenoxy residue was synthesized and evaluated as candidate anticonvulsants. The synthesis was achieved through reaction of 2,3-dichloroquinoxaline (1) with an equimolar amount of 4-aminoacetophenone to give compound 2 which is considered as an important synthon for the construction of a pyridine ring via several synthetic routs. Some compounds were synthesized through formation of the intermediate α,β-unsaturated compounds which, in turn, were allowed to react with malononitrile to give the corresponding alkoxypyridines (8-17). Compounds 18-21 were synthesized by a one-pot simple reaction between 2, the appropriate aldehyde, and malononitrile in sodium alkoxide solution. Moreover, they can be synthesized through reaction of compound 2 and arylidenemalononitrile in sodium alkoxide. The phenoxy analogues were prepared by reaction of 1 with 4-hydroxyacetophenone or 3-hydroxybenzaldehyde to give 22 and 27, respectively. These compounds, in turn, were allowed to react with malononitrile and the proper carbonyl compound in presence of sodium alkoxide in a one-pot reaction technique to give the target compounds. Biological evaluation of the prepared compounds showed that some of them are potent anticonvulsant agents. The detailed synthesis, spectroscopic and biological data are reported

Post Stroke Hyperglycemia as a marker of Stroke Severity and Prognosis: A cohort study

Abstract Background Stroke is the third most leading cause of death worldwide after coronary heart disease and cancer especially ischemic infarcts. Hyperglycaemia is common in patients with acute stroke, occurring in up to 60% of patients overall and approximately 12–53% of acute stroke patients without a prior diagnosis of diabetes, Aim of the Work The aim of this work is study of the glycemic status after acute stroke and assess the role of glycemic status in influencing stroke outcome. Patients and Methods This was a prospective cohort study conducted in the Critical Care Department of Ain-Shams University Hospitals and Damanhour Medical National Institute for six months from January 2018 to June 2018. Conclusion From our study we can conclude that diabetes mellitus as a risk factor in cases of stroke leads to increase complications and worsens the outcome in cases of stroke whether hemorrhagic or ischemic. Recommendations From our study we recommended strict control of diabetes mellitus when present in cases of stroke to avoid bad outcome and to prevent complications in these cases. </jats:sec

Synthesis and antitumor testing of certain new fused triazolopyrimidine and triazoloquinazoline derivatives

AbstractNew series of 1,2,4-triazolopyrimidine and 1,2,4-triazoloquinazoline derivatives were designed, synthesized, and evaluated for their antitumor activity. Compounds 6, 11, 26, 29, 41, 44, 48, 49 and 58 were tested as antitumor agents by the use of DNA-binding assay on TLC-plates, colorimetric assay for the degree of DNA-binding (Methyl green-DNA displacement assay), evaluation of antineoplastic activity against Ehrlich Ascites Carcinoma in mice, and finally modulation of apoptosis. 5-Flurouracil, vitamin C and ethidium bromide were used as positive controls in these techniques. Compound 26 proved to be the most active member of these series as antitumor agent with IC50 value of 47±1. Several characteristic features were observed to be essential for activity such as the morpholine group and the phenylazo group, in addition the electron-withdrawing groups favor the activity than the electron-donating ones