الفهرس 
INTRODUCTIONOnly 14 pages are availabe for public view
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Abstract
This Thesis Comprises Five Chapters:
The First One Is An Introduction Which Consists Of A Brief Survey Of Different Methods For The Synthesis Of 1,2,4-Triazole And Fused Triazole Derivatives, Biological View Of Inflammation And Anti-Inflammatory Drugs, And Recently Reported Triazole And Fused Triazole Derivatives As Anti-Inflammatory Agents.
The Second Chapter Deals With The Objectives Of This Study, The Designs, And Schemes For The Preparation Of The Target Compounds.
The Third Chapter Clarifies The Theoretical Discussion Of The Experimental Work For The Preparation Of Starting Materials (I, II, VIII, Xia,B, And XXI), The Intermediates (III, Iva,B, Xiia,B, Xiiia,B, Xva,B, And Xviiia,B), In Addition To The Synthesis Of The Target 1,2,4-Triazole Derivatives (Va,B, Via-D, Viia-F, Ixa,B, Xa,B, Xiva,B, Xvia,B, Xviia,B, Xixa,B, Xxa-F, And Xxiia-F).
The Synthesis Of Monosubstituted Thiosemicarbazide Derivative III Was Furnished By The Reaction Of II With Potassium Thiocyanate. The Reaction Of Thiosemicarbazide III With Benzoyl Chloride Or P-Toluoyl Chloride Afforded Compounds Iva,B. Dehydrative Cyclization Of Iva,B Into 1,2,4-Triazole-3-Thiol Derivatives Va,B Was Operated.
Also, 1,2,4-Triazole-3-Thiol Derivatives Va,B Were Alkylated With Alkyl Iodide To Get The S-Alkyl Compounds Via-D. Solution Of Sodium Salts Of Va,B In Absolute Ethanol Was Converted Into The Corresponding Ethyl Ester Derivatives Viia–F By The Reaction With Different Ethyl Chloroalkanoate Derivatives. Also, 1,2,4-Triazol-3-Thioacetamide Derivatives Ixa,B Were Synthesized Via The Reaction Of Va,B With N-(4-Acetylphenyl)-2-Bromoacetamide (VIII) In The Presence Of Sodium Metal.
Oxime Derivatives Xa,B Were Prepared By Heating Ketone Derivatives Ixa,B With Hydroxylamine Hydrochloride.
The Starting Compounds Ethyl Pyrazole-4-Carboxylate Derivatives Xia,B Were Reacted With Hydrazine Hydrate Giving The Hydrazide Compounds Xiia,B. New 1,2,4-Triazoles Xiva,B Were Synthesized Through The Reaction Of The Carbohydrazides Xiia,B With Ammonium Thiocyanate To Get The Novel Thiosemicarbazides Xiiia,B, Followed By Intramolecular Cyclization Into Xiva,B.
N-Phenylhydrazine-1-Carbothioamide Derivatives Xva,B Were Obtained By Subjecting The Carbohydrazides Xiia,B To React With Phenylisothiocyanate. Cyclization Of The Carbothioamides Xva,B Was Achieved To Get The New 4-Phenyl-1,2,4-Triazole-3-Thiol Derivatives Xvia,B. Alkylation Of Xvia,B Using Iodomethane Yielded Compounds Xviia,B.
Also, 1,3,4-Oxadiazoles Xviiia,B Were Synthesized Through Treatment Of Hydrazides Xiia,B With Carbon Disulfide. Then, Oxadiazoles Xviiia,B Were Converted Into The 4-Amino-1,2,4-Triazole-3-Thiol Derivatives Xixa,B By Reaction With Hydrazine Hydrate.
A Novel Series Of Schiff Bases Xxa-F Were Prepared By The Reaction Of Xixa,B With Different Aryl Aldehydes. The Synthesized Schiff Bases Xxa-F Were Reacted With 4-Bromophenacyl Bromide (XXI) To Obtain The Target Triazolothiadiazine Compounds Xxiia-F.
In Addition, A Discussion Of The In-Vitro And In-Vivo Anti-Inflammatory Results, Ulcerogenic Liability, And Stomach Histopathological Examination Was Carried Out. Moreover, The Cardiovascular Effect Of The Most selective Compound Xiva In Comparison To Celecoxib Was Illustrated. Docking Study, ADME Profiling, And Conclusion Of The Results Were Included.
The Fourth Chapter Consists Of The Experimental Part Of This Study. The Structure Elucidation Of The New Compounds Was Supported By Elemental Analysis, IR, 1H NMR, 13C NMR In Addition To Mass Spectral Data. It Also Sheds The Light On The In-Vitro COX-1 And COX-2 Inhibitory Activities Of The Newly Synthesized Compounds Compared To Celecoxib And Indomethacin. The Results Of The In-Vivo Anti-Inflammatory Activity Of The Most selective Compounds (Va, Vib, Viia, Xa, Xiva, Xvib, Xxe, Xxiic, And Xxiie), The Ulcerogenic Liability, And The Stomach Histopathological Studies Compared To Celecoxib And Indomethacin Were Mentioned. Moreover, The Cardiovascular Effect Of The Most selective Compound Xiva Was Indicated.
Furthermore, It Contains Detailed Steps For The Docking And ADME Studies.
The Fifth Chapter Includes 190 References from 1923 To 2021.