- Use of miconazole and derivatives thereof as TGR5 agonists (by machine translation)
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The invention belongs to the technical field of medicines, and relates to novel application TGR5 of miconazole and derivatives thereof in treatment, of diseases and conditions of a biological pathologic process involved in treatment, and. The miconazole and the analogues thereof can activate TGR5 active, for use TGR5 in the treatment or prevention of diseases associated with, activity modulation. (by machine translation)
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- Synthesis and evaluation of novel benzene-ethanol bearing 1,2,4-triazole derivatives as potential antimicrobial agents
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The azole pharmacophore is still regarded as a viable lead structure for the synthesis of more efficacious and broad-spectrum antimicrobial agents. In this study, a novel series of triazole derivates that are structurally related to the famous antimicrobial azole pharmacophore were synthesized and the structures of them were characterized by spectral (IR, 1H NMR, 13C NMR, and MS spectra) analysis. Antimicrobial activity was measured against both bacteria and fungus. In vitro antimicrobial evaluation showed that five compounds had growth inhibitory effects on the tested Gram-positive bacteria and fungus with special efficacy. Potential antibacterial and antifungal activities are incorporated in these triazole compounds. Results of antimicrobial activities also revealed that compounds (5a–i) were the potent antibacterial and antifungal agents as compared to standard drugs (ciprofloxacin and itraconazole), and thus could be promising new lead molecules.
- Li, Bochao,Zhang, Dawei,Zhang, Yumin,Dan Jiang,Li, Shuang,Lei, Wei,Wang, Huiying,Lin, Feng
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- Aromatic ethers of 1-aryl 2-(1H-azolyl)ethanol: study of antifungal activity
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Aromatic ethers related to antifungal azole miconazole were synthesized and tested against various strains of Candida.We found that activity is related to the nature of the aromatic ring and the position of substituents on this ring.Activity is more strongly dependent on the substituent in the 2-position of the ethyl chain on the aromatic group linked through the oxygen.Triazoles were always less potent than the corresponding imidazole analogues. - Keywords: imidazole; 1,2,4-triazole; antifungal activity; yeast; structure-activity relationship
- Wahbi, Y.,Caujolle, R.,Tournaire, C.,Payard, M.,Linas, M. D.,Seguela, J. P.
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p. 955 - 962
(2007/10/03)
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- Fungicidal 1-phenyl-2-(1,2,4-triazol-1-yl)-ethyl ethers
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1-Phenyl-2-(1,2,4-triazol-1-yl)-ethyl ethers of the formula STR1 in which R is halogen, alkyl, alkoxy, alkylthio, alkylsulfonyl, halogenoalkyl, nitro, cyano, optionally substituted phenyl or optionally substituted phenoxy, R' is alkyl, alkenyl, alkynyl, optionally substituted phenyl, optionally substituted benzyl or optionally substituted styryl, and n is 0, 1, 2 or 3, and their salts, which possess fungicidal and bactericidal properties.
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- 1-Phenyl-2-(1,2,4-triazolyl-1-yl)-ethyl ether
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1-Phenyl-2-(1,2,4-triazol-1-yl)-ethyl ethers of the formula STR1 in which R is halogen, alkyl, alkoxy, alkylthio, alkylsulfonyl, halogenoalkyl, nitro, cyano, optionally substituted phenyl or optionally substituted phenoxy, R' is alkyl, alkenyl, alkynyl, optionally substituted phenyl, optionally substituted benzyl or optionally substituted styryl, and n is 0, 1, 2 or 3, and their salts, which possess fungicidal and bactericidal properties.
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