Synthesis of Mercapto-(Oxadiazole/Triazole) Carboxylic acid Compounds and their derivatives of Biological interest

Abstract

The research work reported in this dissertation consists of synthesis of newlinepharmacologically active compounds and the modification of their structure according to the result of pharmacological screening. All these synthesized compounds were characterized by satisfactory spectroscopic data. These compounds belongs to the classes of 1,3,4-oxadiazole-2(3H)-thione and 1,2,4- newlinetriazole-3(4H)-thione. All these compounds were screened for different biological newlineactivities including bactericidal, fungicidal, analgesic, anti-inflammatory, newlineanxiolytic and anticonvulsant activities and as expected most of them had exhibited moderate to good activities. Scheme I and Scheme II: Here focus was made mainly on the synthesis of 1,2,4- triazoline-3-thione as the essential pharmacophore and investigation of its combination with various N-substituted carboxamidoalkylthio moiety through sulfur atom and converting them to corresponding sulfoxides and sulfones selectively by solid state green oxidation method using Oxone®. newlineAnalgesic and Anti-inflammatory activity: All the synthesized triazole derivatives (11a-k) were found to exhibit potent anti-inflammatory activity but lower analgesic activity as compared to (6a-k). It might be due to increase in distance between aromatic nucleus and side chain nitrogen by one carbon atom as to exhibit analgesic activity, molecule should contain one aromatic nucleus newlineattached to quaternary carbon then ethylene bridge and tertiary nitrogen. N-Phenyl newlinecarboxamidoethylthio-(4H)-1,2,4-triazole (11a) had exhibited equipotent antiinflammatory newlineand analgesic activity as compared to standard drug. Anxiolytic Activity: All the compounds (6a-k and 11a-k) were tested for their Anxiolytic activity. There was increase in percent time spent and number of entries newlinein the open arm but the Anxiolytic activity was found to be very less as compared newlineto diazepam.