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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.

The mycotoxin ochratoxin A (OTA) is a widespread contaminant in human and animal food products. It induces a wide range of toxic effects including lipid peroxidation through the generation of free radicals. The aim of this work was to evaluate the antioxidant effects of melatonin against OTA-induced oxidative stress in liver and kidney in rats. Treated animals were fed OTA-contaminated diet (3 mg/kg) for 15 days before, during and after melatonin administration (20 mg/kg bw). The results indicate that OTA caused severe effects typical to those reported in the literature for ochratoxicosis. Melatonin alone was effective in the improving food intake, body weight gain, serum total protein, albumin, the activities of alkaline phosphatase, G-glutamyl transferase and creatinine kinase and liver and kidney glutathione peroxidase, superoxide dismutase and malondialdehyde. Rats fed OTA-contaminated diet before, during or after melatonin administration showed a significant improvement in all tested parameters toward the normal values of the controls. This improvement was most pronounced in the group pretreated with melatonin. It is concluded that melatonin exhibits a preventive effect against OTA-induced oxidative stress through its role in the scavenging of free radicals and/or the prevention of lipid peroxidation.

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Some chromeno[4,3-b]quinolines 4a-i were obtained from beta-chloro carboxyaldehydes 3a-c with different aniline derivatives namely, aniline, 4-fluoroaniline, and 2-aminophenol. Surprisingly, 3a-c reacted with 2-aminothiophenol and afforded the chromeno[3,4-c]quinoline derivatives 5a-c. Single-crystal X-ray diffraction studies of 4e and 5b provided good support for the established structure. Compounds 4b and 5b showed significant anti-inflammatory and ulcerogenic score activities compared to that of indomethacin.

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Some new tetrahydropyrimidine-2-thione, octahydroquinazoline-2-thione and thiazolo[3,2-a]pyrimidine derivatives have been synthesized and tested for their antihypertensive activity. Among them, compounds 1 and 2b can be considered more potent than the reference, nifedipine (CAS 21829-25-4), while compounds 3b and 10a are equipotent to it. In addition, compound 6 showed significant antihypertensive activity.