SYNTHESIS AND BIOLOGICAL SCREENING OF A NOVEL CLASS OF POTENTIAL ANTI-INFLAMMATORY AGENTS

Somashekhar M.* and R. B. Kotnal

ABSTRACT

A series of novel 5[4-Morpholin-4-yl-Phenyl)-1, 3, 4-oxadiazole 2-thiol were synthesized by the morpholie and 4-chloro-benzonitrile on reflux gives 4-(morpholine-4-yl) benzonitrile. This upon treating with sodium hydroxide gives 4-(morpholin-4-yl) benzoic acid. Then this upon treating with thionyl chloride gives 4-(morpholin-4-yl) benzoyl chloride. This on further treatment with hydrazine-hydrate gives 4-(morpholin-4-yl) benzohydrazide which is treated for cylcisation with carbon disulphide in presence of potassium hydroxide gives resultant compound 5[4-Morpholin-4-yl-Phenyl)-1,3,4-oxadiazole 2-thiol then it is treated with various substituted to form 1, 3, 4-oxadiazole derivatives. Hydrazides were synthesized so as to increase intracellular concentration and so as to try and decrease the resistant developed due to decrease intracellular concentration of the drug. These synthesized compounds were subjected to preliminary biological evaluation. The characterization of synthesized compounds was identified on the basis of IR, 1HNMR, Mass spectroscopy. The compounds have been evaluated for anti-inflammatory activity.

Keywords: Morpholine, P-Chlorobenzonitrile, 1, 3, 4-Oxadiazole, Anti-inflammatory activity.