- IMIDAZOLE-BASED ANTICANCER AGENTS AND DERIVATIVES THEREOF, AND METHODS OF MAKING AND USING SAME
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Imidazole-based anticancer agents and derivatives thereof, as well as methods of making and methods of using the same, are described. The imidazole-based anticancer agents are HDAC inhibitor compounds having a 1-(1H-imidazol-2-yl)ethan-1-one or 1-(1H-imidazol-2-yl)ethane-1- thione moiety.
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Paragraph 0048-0049
(2019/03/05)
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- Gas-phase pyrolysis in organic synthesis: New route for synthesis of functionally substituted imidazoles
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(Chemical Equation Presented) 1,2,3-Triazolylpropanone was prepared and coupled with aryldiazonium salts yielding the corresponding arylhydrazones. Gas-phase pyrolysis of the hydrazono derivative produced N-arylamino-2- acetylimidazole as well as 2-acetyl
- El-Dusouqui, Osman M. E.,Abdelkhalik, Mervat M.,Al-Awadi, Nouria A.,Elnagdi, Mohamed H.
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experimental part
p. 1751 - 1753
(2009/05/31)
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- PYRAZOLE DERIVATIVE
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A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
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Page/Page column 60-61
(2010/11/27)
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- ARYLOXY-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES
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A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.
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Page/Page column 70
(2010/11/28)
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- PYROLISE-ECLAIR EN PHASE GAZEUSE DU 1-ACETYLIMIDAZOLE.
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1-acetylimidazole is isomerized into 2- and 4-acetylimidazoles and under flash-vacuum pyrolytic conditions.This has been demonstrated by a real-time analysis of the products using mass and ion kinetic energy spectrometries.
- Maquestiau, A.,Tommasetti, A.,Pedregal-Freire, C.,Elguero, J.,Flammang, R.
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p. 1067 - 1072
(2007/10/02)
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- 2-GUANIDINO-4-HETEROARYL-THIAZOLES
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A series of 2-guanidino-4-heteroarylthiazoles, wherein the heteroaryl substituent is selected from thiazolyl, triazolyl, imidazolyl, and 2-alkyl, 2-amino and 2-carboxamido derivatives thereof, are disclosed. The novel compounds have activity as antisecretory agents and histamine H 2 antagonists and are useful for the treatment of gastric hyperacidity and peptic ulcers. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of using the compounds in the treatment of gastric hyperacidity and peptic ulcers. Novel intermediates useful in the preparation of the novel antisecretory compounds are also described.
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- An Easily Introduced and Removed Protecting Group for Imidazole Nitrogen: A Convenient Route to 2-Substituted Imidazoles
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Orthoamides (3-5) prepared from imidazoles and triethyl or trimethyl orthoformate are rapidly metalated at -40 deg C in THF or ether to give the corresponding 2-lithio anion which reacts with a variety of electrophiles.The dialkoxymethyl protecting group is readily hydrolyzed under neutral or acidic conditions at room temperature, giving the 2-substituted 1H-imidazole 1 (R = H, X = COOH, n-C4H9, COCH3, CHOHC6H5, C(CH3)OH-2-pyridyl,9-hydroxyfluorenyl, 1-hydroxycyclohex-2-enyl, C(OH)(C6H5)2; R = CH3, R' = H, X = CHO) and the tris(2-imidazolyl)phosphines (R = H, CH3, CH(CH3)2).A mechanism for the deprotection of 3 is proposed.
- Curtis, N.J.,Brown, R.S.
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p. 4038 - 4040
(2007/10/02)
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