- Structure–activity relationships and docking studies of hydroxychavicol and its analogs as xanthine oxidase inhibitors
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Hydroxychavicol (HC), which is obtained from the leaves of Piper betle LINN. (Piperaceae), inhibits xanthine oxidase (XO) with an IC50 value of 16.7μM, making it more potent than the clinically used allopurinol (IC50=30.7μM). Herein, a structure–activity relationship analysis of the polar part analogs of HC was conducted and an inhibitor was discovered with a potency 13 times that of HC. Kinetic studies have revealed that HC and its active analog inhibit XO in an uncompetitive manner. The binding structure prediction of these inhibitor molecules to the XO complex with xanthine suggested that both compounds (HC and its analog) could simultaneously form hydrogen bonds with xanthine and XO.
- Nishiwaki, Keiji,Ohigashi, Kanae,Deguchi, Takahiro,Murata, Kazuya,Nakamura, Shinya,Matsuda, Hideaki,Nakanishi, Isao
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p. 741 - 747
(2018/07/05)
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- A highly efficient metal-free approach to: Meta - And multiple-substituted phenols via a simple oxidation of cyclohexenones
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A novel and efficient metal-free approach to substituted phenols has been disclosed from simple and readily available cyclohexenones and cyclohexenone equivalents. Dimethyl sulfoxide (DMSO), a simple and common organic reagent, was employed as a mild oxidant in this I2-catalysis, which significantly tolerates various substituents including some easily oxidizable or reducible functionalities. The challenging meta- and multiple-substituted phenols could be well prepared by this method. The metal-free and mild oxidation make this protocol very simple, practical, and easy to handle.
- Liang, Yu-Feng,Song, Song,Ai, Lingsheng,Li, Xinwei,Jiao, Ning
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supporting information
p. 6462 - 6467
(2018/06/08)
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- ASPARTYL PROTEASE INHIBITORS
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The invention provides compounds of the formula (I) N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein G is-O-, -S(=O)r-, -CRdRd or -NRa-; W is H, C1-C6
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- Mild debenzylation of aryl benzyl ether with BCl3 in the presence of pentamethylbenzene as a non-lewis-basic cation scavenger
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Scope and limitations of the debenzylation conditions for aryl benzyl ether, which was developed during our synthetic studies on yatakemycin, were investigated. The chemoselective debenzylation proceeds at low temperature with a combination of BCl3 and pentamethylbenzene as a cation scavenger in the presence of various functional groups.
- Okano, Kentaro,Okuyama, Kei-Ichiro,Fukuyama, Tohru,Tokuyama, Hidetoshi
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scheme or table
p. 1977 - 1980
(2009/04/07)
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- The synthesis of phenolic propane-1, 2- and 1,3-diols as intermediates in immobilised chelatants for the borate anion
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The isomeric 3-(hydroxyphenyl)propane-1, 2-diols have been synthesised from allylic precursors by epoxidation and cleavage. Several different methods have been examined for obtaining 1-(methoxyphenyl)propane-1, 3-diols. 2-(methoxyphenyl)propane-1, 3-diols and certain hydroxy analogues have been obtained from benzaldoximes converted by oxidation to methoxy- and benzyloxynitromethylbenzenes followed by hydroxymethylation with formaldehyde and catalytic hydrogenation.
- Tyman, John H. P.,Payne
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p. 691 - 695
(2007/10/03)
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