Imidazole Derivatives Biological Activity And Synthetic Approaches
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My seminar presentation at Dept. of Medicinal Chemistry, NIPER.
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Imidazole Derivatives Biological Activity And Synthetic Approaches
- 1. Imidazole Derivatives : Biological Activity And Synthetic Approaches
- 8. Antithyroid drugs :- Thyroid Peroxidase Murray, R. K. et al. In Harper's Illustrated Biochemistry . 26 th ed. 2003; pp 447-449. Clinical use :- conditions of hyperthyroidism such as Grave’s disease, toxic uninodular / multinodular goiter, thyroid storm etc. - Biological activity of synthetic imidazole derivatives
- 14. Mechanism of proton pump inhibition :- Clinical use :- Anti-ulcer drugs Lindberg, P. et al. J. Med. Chem. 1986, 29 , 1327-1329. Parietal cells in stomach-wall Excitatatory nerve-signal by ANS Activated parietal cell Gastric acid secretion Histamine Enzyme H + K + - ATPase pump - Biological activity of synthetic imidazole derivatives
- 16. Eicher, T. et al. In The Chemistry of Heterocycles:Structure, Reactions, Syntheses and Applications . 2nd ed.; WILEY-VCH GmbH & Co.: Weinheim, 2003; pp 170-172. Retrosynthetic analysis for imidazole
- 17. The pioneer synthesis :- By this route, imidazole was first synthesized by H. Debus in 1858 from glyoxal, ammonia and formaldehyde, and was known as “glyoxaline”. Debus, H. Ann. Chem. 1858, 107 , 199 Conventional methods for imidazole synthesis
- 18. TosMIC based imidazole synthesis :- Leusen, A. M. et al. J. Org. Chem. 1977, 42 , 1153-1159. Conventional methods for imidazole synthesis
- 19. Synthesis of imidazole from amidines :- Shilcrat, S. C. et al. J. Org. Chem. 1997, 62 , 8449-8454. Conventional methods for imidazole synthesis
- 21. Follow catalytic &/or multicomponent reaction strategies or entirely different concept such as reaction by EMR irradiation. -: Catalytic reactions for imidazole synthesis :- Synthesis of imidazoles by modern methods
- 22. Palladium-catalyzed intramolecular cyclization reaction :- Zaman, S. et al. Org. Lett. 2005, 7 , 609-611. -: Palladium catalyzed syntheses :- Synthesis of imidazoles by modern methods
- 23. Palladium catalyzed multicomponent coupling reaction :- Mihovilovic, M. D. et al. Angew. Chem. 2007, 46 , 3612-3615. -: Palladium catalyzed syntheses :- Synthesis of imidazoles by modern methods
- 24. Ag-acetate catalyzed cyclodimerization :- Cu-catalyzed cross-cycloaddition :- -: d 10 metal catalysts :- Grigg, R. et al. Tetrahedron 1999, 55 , 2025-2044. Kanazawa, C. et al. J. Am. Chem. Soc. 2006, 128 , 10662-10663. Synthesis of imidazoles by modern methods
- 25. ZrCl 4 -catalyzed imidazole synthesis :- Ytterbium-triflate catalyzed 3-component condensation :- -: Lewis acids as catalysts :- Sharma, G. V. M. et al. Chem. Inform. 2007, 38 , 2991-2993. Wang, L.-M. et al. J. Flu. Chem. 2006, 127 , 1570-1573. Synthesis of imidazoles by modern methods
- 26. Thiazolium-catalyzed 3-component coupling reaction :- HClO 4 –SiO 2 catalyst for imidazole synthesis :- -: Lewis acids as catalysts :- Frantz, D. et al. Org. Lett. 2004, 6 , 843-846. Nagarapu, L. et al. J. Mol. Catal. 2007, 267 , 53-56. Synthesis of imidazoles by modern methods