- Chemistry of 2-hetarylbenzimidazoles. 10*. Synthesis and properties of 2-(3′-furyl)-1-methyl-1H-benzimidazole
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A study was carried out on the electrophilic substitution reactions such as chloromethylation, bromination, sulfonation, nitration, and acylation of 2-(3′-furyl)-1-methyl-1H-benzimidazole in acid media. All these reactions proceed at C(2) and C(5) of the furan ring. Quantum-chemical calculations of the three-dimensional structure of such heterocyclic systems are given. 2005 Springer Science+Business Media, Inc.
- Achkasova,Elchaninov,Milov,Lukyanov
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- Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection
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Butyrylcholinesterase (BChE) has been considered as a potential therapeutic target for Alzheimer's disease (AD) because of its compensation capacity to hydrolyze acetylcholine (ACh) and its close association with Aβ deposit. Here, we identified S06-1011 (hBChE IC50 = 16 nM) and S06-1031 (hBChE IC50 = 25 nM) as highly effective and selective BChE inhibitors, which were proved to be safe and long-acting. Candidate compounds exhibited neuroprotective effects and the ability to improve cognition in scopolamine- and Aβ1-42 peptide-induced cognitive deficit models. The best candidate S06-1011 increased the level of ghrelin, a substrate of BChE, which can function as improving the mental mood appetite. The weight gain of the S06-1011-treated group remarkably increased. Hence, BChE inhibition not only plays a protective role against dementia but also exerts a great effect on treating and nursing care.
- Li, Qi,Chen, Ying,Xing, Shuaishuai,Liao, Qinghong,Xiong, Baichen,Wang, Yuanyuan,Lu, Weixuan,He, Siyu,Feng, Feng,Liu, Wenyuan,Chen, Yao,Sun, Haopeng
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p. 6856 - 6876
(2021/05/29)
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- 2-heteroaryl benzimidazole derivatives as melanin concentrating hormone receptor 1 (MCH-R1) antagonists
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A novel series of 2-heteroaryl substituted benzimidazole derivatives, containing the piperidinylphenyl acetamide group at the 1-position, were synthesized and evaluated as MCH-R1 antagonists. Extensive SAR investigation probing the effects of C-2 heteroaryl group led to the identification of 2-[2-(pyridin-3-yl)ethyl] analog 3o, which exhibits highly potent MCH-R1 binding activity with an IC50 value of 1 nM. This substance 3o also has low hERG binding activity, good metabolic stability, and favorable pharmacokinetic properties.
- Lim, Chae Jo,Kim, Jeong Young,Lee, Byung Ho,Oh, Kwang-Seok,Yi, Kyu Yang
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p. 2305 - 2310
(2013/09/24)
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- Indium-mediated reductive intermolecular coupling reaction of 2-nitroaniline with aromatic aldehydes to benzimidazoles
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2-Nitroaniline and aromatic aldehydes were coupled to give benzimidazoles in high yields in the presence of 2-bromo-2-nitropropane and indium at room temperature.
- Kim, Byeong Hyo,Han, Rongbi,Kim, Ji Sook,Jun, Young Moo,Baik, Woonphil,Lee, Byung Min
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- Synthesis and Tautomerism of 2-Aryl- and 2-Heteroaryl Derivatives of Benzimidazole
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Benzimidazoles containing furyl and thienyl substituents at C-2 were prepared by condensation of o-phenylenediamine and corresponding carboxylic acids in the presence of polyphosphoric acid. The 2-heteroarylbenzimidazoles showed tautomerism in dimethyl sulfoxide solution while 2-phenylbenzimidazole did not. The tautomerism appeared to be taking place by intermolecular relay of protons between stacked molecules.
- Lee, In-Sook Han,Jeoung, Eun Hee,Lee, Chang Kiu
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p. 1711 - 1716
(2007/10/03)
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