- Method for preparing benzimidazole compound
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The invention discloses a method for preparing a benzimidazole compound, namely 5-methoxyl-2-(4-methylpiperidine-1-yl)-1H-benzo[d]imidazole. The method comprises the following steps of using 5-methoxyl-2-nitroaniline as the initiating raw material, and performing reduction, loop closing, chloridizing and nucleophilic reaction, so as to obtain a target product. The compound is an important medicineintermediate.
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Paragraph 0025-0026
(2018/03/24)
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- Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole derivatives
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Design, syntheses, and structure-activity relationships of a novel class of 2-{3-oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole NPY Y5 receptor antagonists are described. The benzimidazole structures were newly designed based on the urea linkage of our prototype Y5 receptor antagonists (2 and 3). By optimizing substituents on the benzimidazole core part of the lead compound 5a, we were able to develop a potent, orally available, and brain-penetrable Y5 selective antagonist (5k). Crown Copyright
- Ogino, Yoshio,Ohtake, Norikazu,Nagae, Yoshikazu,Matsuda, Kenji,Moriya, Minoru,Suga, Takuya,Ishikawa, Makoto,Kanesaka, Maki,Mitobe, Yuko,Ito, Junko,Kanno, Tetsuya,Ishihara, Akane,Iwaasa, Hisashi,Ohe, Tomoyuki,Kanatani, Akio,Fukami, Takehiro
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scheme or table
p. 5010 - 5014
(2009/05/07)
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- 4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists
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A series of 4-(2-pyridyl)piperazine-1-benzimidazole analogues based on compound 1 was synthesized and evaluated for TRPV1 antagonist activity in capsaicin-induced (CAP) and pH 5.5-induced (pH) FLIPR assays in a human TRPV1-expressing HEK293 cell line. Potent TRPV1 antagonists were identified through SAR studies. From these studies, several antagonists were found, with IC50 values ranging from 32 nM to ~5000 nM. Among these, 11 [IC50 = 90 nM (CAP) and 104 nM (pH)] was further evaluated and found to be orally available in rats (F% = 19.7).
- Shao, Bin,Huang, Jincheng,Sun, Qun,Valenzano, Kenneth J.,Schmid, Lori,Nolan, Scott
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p. 719 - 723
(2007/10/03)
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