This dissertation has been divided into three chapters and each chapter has its own numbering of compounds and references. General introduction of dissertation describing the significance of natural products and natural product-based drugs. This research work describes synthesis and bioactivities of heterocyclic class of compound such as oxadiazole derivatives, Schiff bases of 2,4-dinitrophenyl hydrazine derivatives,bis-Schiff bases of 4,4-bis(dimethylamino)benzophenone and bis-Schiff bases of hydrazides and their analoges in search of important therapeutic agents. During this research study, a varity of oxadiazole derivatives, Schiff bases of 2,4-dinitrophenyl hydrazine derivatives, Bis-Schiff bases of 4,4-bis(dimethylamino)benzophenone, Bis-Schiff bases of hydrazides and theirs related analogs were synthesized and screened for Anti-Cholinesterase, antiacetylcholinesterase (AChE) and anti-butyrylcholinesterase (BChE), antioxidant, and α- Glucosidase activities. The results obtained from this study are encouraging which are discussed separately in chapters 1, 2 and 3. In first chapter, oxadiazole derivatives, an important class of heterocycles, have been described. Oxadiazole derivatives showed a varying degree of anti-cholinesterase activity and butyrylcholinesterase activity. Out of 31 synthesized analogs, 28 oxadiazole derivatives were found to be potent anti-cholinesterase inhibitory agent except three compounds 147, 164 and 165. Second chapter describes Schiff bases of 2,4-dinitrophenyl hydrazine derivatives. All prepared schiff bases were tested for anti-oxidant activities. During antioxident assays all compounds 128- 160 showed excellent to moderate DPPH free radical scavenging activities. Among the most active analogs, compounds 134, 136, 137, 144 and 160 were found to be the most active agents, six compounds 128, 135, 139, 140, 148 and 158 were found active against Ferrous ion-chelation activity, three compounds 133, 137 and 154 were found to have Ferric ion reducing activity, five anologes 146, 154, 155, 156 and 159 were active in vitro total antioxidant activity while three compounds 137, 155, 159 also showed better hydroxy radical scavenging activity. Third chapter describes one of the most important class of Bis-Schiff bases i.e. bis-Schiff base of 4,4-bis(Dimethylamino)benzophenone and bis-Schiff bases of hydrazides. A novel of bis-Schiff base of 4,4-bis(Dimethylamino)benzophenone has been synthesized and screened for their in vitro antioxidant activitiy. All the synthetic analogs 69-95 were subjected to in vitro antioxidant activity, by using rapid and simple antioxidant assays such as DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging, ferrous ion-chelating, ferric reducing/antioxidant power assay, total antioxidant activity by phasphomolabdenum method and hydroxy radical scavenging assay. Once again, results were found to be intresting and all compounds were demonstrated good to weak antioxidant activities. These compounds were also tested for their α-Glucosidase inhibition activity, which showed above 50% inhibition except compounds 79, 88, 89, 93, and 95. Prepared compounds were subjected to anti-cholinesterase activity, and displayed weak to moderate inhibition. bis-Schiff bases of hydrazides 129-160 were also checked for in-vitro antioxidant activities by different asssays. Out of 32 analogs four compounds 139, 141, 147 and 148 showed moderate, while rest of the compounds showed good to weak DPPH radical scavenging activity. Further rmore, these analoges were also tested for anti-cholinesterase activity, three compounds 142, 149 and 150 exitbhited an excellent activity.
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