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Synthesis and biological testing of 1-adamantyl derivatives
English
208 b
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Several adamantane derivatives have long been known for diverse biological properties, mainly as antiviral, antibacterial, antifungal and anti-inflammatory agents. adamantyl derivatives were recently reported to possess 11-HSD1 inhibitory activities. In addition, 1,2,4-triazole and 1,3,4-thiadiazole were reported to constitute the pharmacologically active moiety of several compounds. On these bases new series of 1-adamantyl derivatives, in which the adamantyl moiety was attached to 1,2,4-triazole, 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole or 1,3,4-thiadiazole nucleus, have been synthesized as potential bioactive agents All the synthesized compounds were tested for their in vitro growth inhibitory activity against a panel of standard strains of pathogenic microorganism including Gram-positive bacteria, Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. In addition, the acute anti-inflammatory activity of a representative compounds was determined in vivo following the carrageenan-induced paw oedema method in rats.
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