Microwave-assisted synthesis of new benzimidazole derivatives with lipase inhibition activity.
作者： Emre Menteşe , Hakan Bektaş , Serdar Ülker , Olcay Bekircan , Bahittin Kahveci
DOI: 10.3109/14756366.2012.753880
关键词:
摘要: A practical protocol has been used for the synthesis of benzimidazoles. The reaction iminoester hydrochlorides phenylacetic with 4,5-dichloro-1,2-phenylenediamine under microwave irradiation leads to benzimidazole derivatives good yields and in short times. After benzimidazoles, we synthesized ester hydrazide yields. All compounds were evaluated regard pancreatic lipase activity 3b, 3c, 5a 6a showed inhibition at various concentrations.
sci-hub.se 参考文章(24)
Robert Verger, Henri Chahinian, Carole Serveau-Avesque, Method for the high-speed detection and/or measurement of a lipase or phospholipase activity ,(2006)
Lucinda M. Dudd, Eleni Venardou, Eduardo Garcia-Verdugo, Peter Licence, Alexander J. Blake, Claire Wilson, Martyn Poliakoff, Synthesis of benzimidazoles in high-temperature water Green Chemistry. ,vol. 5, pp. 187- 192 ,(2003) , 10.1039/B212394K
Jun Lu, Bingqin Yang, Yinjuan Bai, Microwave irradiation synthesis of 2-substituted benzimidazoles using PPA as a catalyst under solvent-free conditions Synthetic Communications. ,vol. 32, pp. 3703- 3709 ,(2002) , 10.1081/SCC-120015381
Luc F. Van Gaal, Ilse L. Mertens, Christophe E. De Block, Mechanisms linking obesity with cardiovascular disease Nature. ,vol. 444, pp. 875- 880 ,(2006) , 10.1038/NATURE05487
Benay Can-Eke, M. Orhan Puskullu, Erdem Buyukbingol, Mumtaz Iscan, A study on the antioxidant capacities of some benzimidazoles in rat tissues. Chemico-Biological Interactions. ,vol. 113, pp. 65- 77 ,(1998) , 10.1016/S0009-2797(98)00020-9
A. Hunger, J. Kebrle, A. Rossi, K. Hoffmann, Benzimidazol‐Derivate und verwandte Heterocyclen VI. Synthese von Phenyl‐[1‐aminoalkyl‐benzimidazolyl‐(2)]‐essigsäure‐estern und ‐amiden Helvetica Chimica Acta. ,vol. 43, pp. 1727- 1733 ,(1960) , 10.1002/HLCA.19600430634
Peter Köhler, The biochemical basis of anthelmintic action and resistance. International Journal for Parasitology. ,vol. 31, pp. 336- 345 ,(2001) , 10.1016/S0020-7519(01)00131-X
Hiroyuki Nakano, Tsutomu Inoue, Nobuhide Kawasaki, Hideki Miyataka, Hitoshi Matsumoto, Takeo Taguchi, Naoki Inagaki, Hiroichi Nagai, Toshio Satoh, Synthesis and biological activities of novel antiallergic agents with 5-lipoxygenase inhibiting action. Bioorganic & Medicinal Chemistry. ,vol. 8, pp. 373- 380 ,(2000) , 10.1016/S0968-0896(99)00291-6
Gui-Dong Zhu, Viraj B. Gandhi, Jianchun Gong, Sheela Thomas, Yan Luo, Xuesong Liu, Yan Shi, Vered Klinghofer, Eric F. Johnson, David Frost, Cherrie Donawho, Ken Jarvis, Jennifer Bouska, Kennan C. Marsh, Saul H. Rosenberg, Vincent L. Giranda, Thomas D. Penning, Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent Bioorganic & Medicinal Chemistry Letters. ,vol. 18, pp. 3955- 3958 ,(2008) , 10.1016/J.BMCL.2008.06.023
Kavitha C.S. Achar, Kallappa M. Hosamani, Harisha R. Seetharamareddy, In-vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives. European Journal of Medicinal Chemistry. ,vol. 45, pp. 2048- 2054 ,(2010) , 10.1016/J.EJMECH.2010.01.029