Treatment of 2-bromoacetylbenzofuran (2) with pyridine afforded its corresponding pyridinium bromide 3. The latter salt reacted with some activated alkenes and acetylenes to give the corresponding indolizine derivatives. Treatment of the salt 3 with benzylidenemalononitriles 9 afforded polysubstituted aniline derivatives, however with arylidenecyanothioacetamides 15 it gave the corresponding 4,5-dihydrothiophenes. Bromide 3 also coupled with p-chlorobenzenediazonium salt followed by ammonium acetate to give the corresponding 1,2,4,5-tetrazine derivative. The biological activity of the newly synthesized compounds was examined and some of them were found to possess anticonvulsant and anti-inflammatory activities.
In clinical practice, the attention given to sexual problems in patients with end-stage renal disease is low. In order to evaluate the erectile function in chronic renal failure patients undergoing hemodialysis (HD) as a renal replacement therapy in upper Egypt, we used the abridged version of the International Index of Erectile Function (IIEF-5). In all, 75 HD patients were subjected to clinical and laboratory investigations. The controls were 948 healthy males representing the general Egyptian population. The prevalence of erectile dysfunction (ED) among the HD patients was 82.5% compared to 30% among controls. The prevalence of ED in HD group was significantly higher than in controls. The prevalence of ED in HD patients o50 y was 80% and it was 88% in those Z50 y, while the prevalence of ED among controls was 28 and 69.8%, respectively. The prevalence of severe degree of ED was significantly higher in both groups compared to controls, while moderate degree of ED showed a statistical significance compared to controls in age groups o50 y and mild degree of ED showed a statistical significance compared to controls in age groups Z50 y. The univariate logistic regression analysis showed that age (r ¼ À0.3368, Po0.01), serum urea (r ¼ À0.5974, Po0.001), and creatinine level (r ¼ À0.5804, Po0.001) have a significant negative correlation with the presence of ED among HD patients, while serum hemoglobin (r ¼ 0.3396, Po0.001) and years of HD age (r ¼ 0.3147, Po0.01) have a significant positive correlation with the presence of ED among the HD patients. In view of the observed high prevalence of ED among the HD patients, we believe that a complete health evaluation of male HD patients should include a discussion about erectile function in the standard clinical care program of patients with renal disease.
Ethyl 2,4-dioxo-4-(p-chloro)phenylbutyrate 2 obtained by condensation of 4-chloroacetophenone with diethyl oxalate was converted to 5-(4-chlorophenyl)-1-phenyl-1H-pyrazole-3-carbohydrazide 5 and 5-(4-chlorophenyl)isoxazole-3-carbohydrazide 6 in good yields. Treatment of 5 or 6 with phenylisothiocyanate and reaction of the resulting thiosemicarbazide 7 or 8 with chloroacetic acid and 4-fluorobenzaldehyde, phenacyl bromides gave the corresponding 4-thiazolidinone 9 or 10 or 1,3-thiazoles 11 or 12, respectively. While the intramolecular cyclization of 7 or 8 in concentrated sulfuric acid afforded 1,3,4-thiadiazoles 13 or 14. The reactivity of hydrazide 5 or 6 towards fluorinated aldehyde, hydrazonoyl chloride, and b-ketoester was studied to give fluorinated hydrazones, bishydrazones, and pyrazoles 15-23. The newly synthesized compounds were screened for their antiviral activity, and compound 19 reduced the number of viral plaques of Herpes simplex type-1 (HSV-1) by 69%. The detailed synthesis and spectroscopic and biological data are reported.
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