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|Title: ||Synthesis, antimicrobial, and anti-inflammatory Synthesis, antimicrobial, and anti-inflammatory activities of novel
|Authors: ||Kadi, Adnan A.|
El-Brollosy, Nasser R.
Al-Deeb, Omar A.
Habib, Elsayed E.
Ibrahim, Tarek M.
El-Emam, Ali A.
|Keywords: ||Adamantyl derivatives|
|Issue Date: ||2007 |
|Publisher: ||Elsevier Masson SAS|
|Citation: ||European Journal of Medicinal Chemistry: 42; 235-242|
|Abstract: ||Reaction of 1-adamantanecarbonyl chloride with certain carboxylic acid hydrazides in pyridine yielded the corresponding N-acyl adamantane- 1-carbohydrazide derivatives 3a-j, which were cyclized to the corresponding 2-(1-adamantyl)-5-substituted-1,3,4-oxadiazoles 4a-j via heating with phosphorus oxychloride. Treatment of 1-adamantylisothiocyanate with some carboxylic acid hydrazides in ethanol yielded the corresponding 1-acyl-4-(1-adamantyl)-3-thiosemicarbazides 7a-g, which were cyclized to the corresponding 2-(1-adamantylamino)-5- substituted-1,3,4-thiadiazole derivatives 8-eg. Compounds 4a-j, 7a-g, and 8a-g were tested for in vitro activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Several derivatives produced good or moderate
activities particularly against the tested Gram-positive bacteria Bacillus subtilis. Meanwhile, compounds 4i and 8g displayed marked antifungal activity against C. albicans. In addition, the in vivo anti-inflammatory activity of the synthesized compounds was determined using the carrageenin-induced paw oedema method in rats. The oxadiazole derivatives 4c, 4g, 4i and 4j produced good dose-dependent anti-inflammatory activity.|
|Description: ||Author: 1, From the Department of Pharmaceutical Chemistry, P. O. Box 2457, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia|
|Appears in Collections:||King Saud University Initial Collection|
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