- N-cyclopropyl methoxy imidazole amide derivative and application thereof in antitumor drugs
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The invention belongs to the technical field of medicinal chemistry, and particularly relates to N-cyclopropyl methoxy imidazole amide derivatives, a preparation method and application of the N-cyclopropyl methoxy imidazole amide derivatives as an MEK inhibitor in antitumor drugs. The invention provides an N-cyclopropyl methoxy imidazole amide derivative as shown in a general formula, and geometric isomers or pharmaceutically acceptable salts, hydrates, solvates or prodrugs of the N-cyclopropyl methoxy imidazole amide derivative. The MEK inhibitor provided by the invention has specificity and effectiveness, and has a wider development prospect. Experimental results show that the N-cyclopropyl methoxy imidazole amide derivative synthesized by the research group has a prospect of developing targeted antitumor drugs.
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- Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists
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TGR5 is emerging as an important and promising target for the treatment of diabetes, obesity and other metabolic syndromes. A series of novel 1-benzyl-1H-imidazole-5-carboxamide derivatives was designed, synthesized and evaluated in vitro and in vivo. The
- Zhao, Shizhen,Li, Xinping,Wang, Le,Peng, Wenjing,Ye, Wenling,Li, Weiguo,Wang, Yan-Dong,Chen, Wei-Dong
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- Synthesis of 1-benzyl-8,9-dihydroimidazo[4,5-c]pyrrolo[3,2-g]quinolin-4(5H) -one via palladium-catalyzed intramolecular arylation
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The synthesis of a novel tetracyclic structure, 8,9-dihydroimidazo[4,5-c] pyrrolo[3,2-g]quinolin-4(5H)-one, has been achieved by a convergent pathway. Coupling of the weakly nucleophilic hindered aromatic amine with 1-benzylimidazole-4-carboxylic acid, 7, afforded the corresponding amide 9 using a DCP/DMF complex; subsequent Heck-type arylation leading to desired tetracyclic molecule imidazo[4,5-c]-pyrrolo[3,2-g]quinolin-4(5H)-one.
- Delest, Bruno,Tisserand, Jean-Yves,Robert, Jean-Michel,Nourrisson, Marie-Renée,Pinson, Patricia,Duflos, Muriel,Le Baut, Guillaume,Renard, Pierre,Pfeiffer, Bruno
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p. 6079 - 6083
(2007/10/03)
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