SYNTHESIS, BIOLOGICAL EVALUATION AND ANALYTICAL STUDIES OF SOME HETEROCYCLIC COMPOUNDS

Abstract

Inflammatory diseases are widely prevalent throughout the world.Anumber ofnon steroidal antiinflammatory drugs (NSAIDs)are used to relieve pain, supress swelling and im prove mobility in these diseases. Such drugs available in the market are phenylbutazone oxyphenbutazone, diclofenac, ibuprofen, indomethacine, benoxaprofen, benorylate, caprofen, ketoprofen etc. Though these drugs are widely used, they continueto be associated with significant toxicity, particularly in the gastrointestinal tract and kidney. As such efforts are being made all over the world to synthesize new and safer antiinflammatory agents. The survey ofliterature reveals that many workers have reported synthesis and antiinflammatory activity ofpyrimidine acridine, thiazole, thiazoline and thiourea derivatives. In this laboratory, the work is being persued for some time to prepare new compounds and screen them for antiinflammatory activity. In continuation of our work in this direction, we have now synthesized a number of mercaptopyrimidines, pynmidobenzimidazoles, acridine and thiazoline derivatives and evaluated them for their antiinflammatory activity. The heterocyclic compounds so prepared have donor atoms and can form complexes with metals. Thus, the synthesized compounds can also be used for metal determination by using them as extractant or colour developing reagents or materials for preparing membranes to be used as ion selective electrodes (ISEs). We have, therefore further investigated the synthesized compounds for their possible use as electroactive materials for preparing membranes to be employed in ISEs. Out oftwenty four compounds synthesized, five could be successfully used as electroactive material for preparing new ISEs which can determine Hg», Cu*. Pd* Pb* and Cd» Thus the present thesis reports synthesis, characterization and antiinflammatory activity evaluation of twenty four heterocyclic compounds and also deals with utilization ofsome ofthe compounds in the preparation ofISEs for analytical purpose. Abriefsummary ofthe results obtained is presented here. Forthe sake ofclarity, the work embodied in this thesis has been divided into five chapters. Chapter-1: It consists ofthree parts-1.1 , 1.2 and 1.3 1.1 Inflammation inhibitors:- It deals with the recent work reported in literature on the synthesis and antiinflammatory activity evaluation ofpyrimidine, acridine, thiazole, thiazoline and thiourea derivatives. 1.2 Heterocyclic compounds as analytical reagents:- Recent work reported in literature on the determination ofHg» Cu» Pd» Pb» and CcP using heterocyclic compounds is described. 1.3 Utilization of heterocyclic compounds as electroactive materials in developing ion selective electrodes:- This part deals with abrief introduction of ion selective electrodes and reviews the recent work on the use ofheterocyclic compounds as electroactive materials for preparing ion selective electrodes for determining metal ions. Chapter - II : This chapter deals with synthesis of mercaptopyrimidines (I-VI) and pynmidobenzimidazoles (VII-X) by following reaction scheme 2.1. 0) ...........................