- Synthesis and Evaluation of Indole-Based Autoinducers on Quorum Sensing in Vibrio cholerae
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Vibrio cholerae (V. cholerae) uses the autoinducer CAI-1 (cholera autoinducer 1) and several linked quorum sensing systems in order to efficiently sense its ever-changing environment and optimally coordinate population-wide gene expression. Indole has been reported as an important signal that is sensed by V. cholerae, and here, we report the synthesis and evaluation of a focused library of synthetic indole-CAI-1 derivatives as tools to probe quorum sensing (QS) in this human pathogen. Our results show interesting and diverging effects for several conjugates, as compared to CAI-1, on virulence factor production and biofilm formation.
- Holoidovsky, Lara,Meijler, Michael M.
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p. 572 - 576
(2020/04/30)
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- Polypyridyl iridium(III) based catalysts for highly chemoselective hydrogenation of aldehydes
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Iridium-catalyzed transfer hydrogenation (TH) of carbonyl compounds using HCOOR (R = H, Na, NH4) as a hydrogen source is a pivotal process as it provides the clean process and is easy to execute. However, the existing highly efficient iridium catalysts work at a narrow pH; thus, does not apply to a wide variety of substrates. Therefore, the development of a new catalyst which works at a broad pH range is essential as it can gain a broader scope of utilization. Here we report highly efficient polypyridyl iridium(III) catalysts, [Ir(tpy)(L)Cl](PF6)2 {where tpy = 2,2′:6′,2′'-Terpyridine, L = phen (1,10-Phenanthroline), Me2phen (4,7-Dimethyl-1,10-phenanthroline), Me4phen (3,4,7,8-Tetramethyl-1,10-phenanthroline), Me2bpy (4,4′-Dimethyl-2–2′-dipyridyl)} for the chemoselective reduction of aldehydes to alcohols in aqueous ethanol and sodium formate as the hydride source. The reaction can be carried out efficiently in broad pH ranges, from pH 6 to 11. These catalysts are air stable, easy to prepare using commercially available starting materials, and are highly applicable for a wide range of substrates, such as electron-rich or deficient (hetero)arenes, halogens, phenols, alkoxy, ketones, esters, carboxylic acids, cyano, and nitro groups. Particularly, acid and hydroxy groups containing aldehydes were reduced successfully in basic and acidic reaction conditions, demonstrating the efficiency of the catalyst in a broad pH range with high conversion rates under microwave irradiation.
- Pandrala, Mallesh,Resendez, Angel,Malhotra, Sanjay V.
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p. 283 - 288
(2019/09/30)
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- RORγ MODULATORS
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The invention provides an RORγ receptor agonist comprising a compound of formula (I), wherein the variables are as defined herein. These compounds are analogous to known RORγ receptor antagonists. The invention further provides a method of activating -the nuclear receptor RORγ, comprising -contacting the RORγ with an effective amount or concentration of a compound of the invention; and a method of treating cancer in a patient, comprising administering to the patient an effective dose of a compound of the invention.
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Page/Page column 20-21; 23-24; 31
(2018/04/13)
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- NEAR-INFRARED-ABSORBING DYE, OPTICAL FILTER, AND IMAGING DEVICE
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Provided is a near-infrared-absorbing dye increasing a visible light transmittance and having a near-infrared blocking characteristic. The near-infrared-absorbing dye has an absorption characteristic measured by dissolving the dye in dichloromethane satisfying the following requirements. ?In an absorption spectrum at a wavelength of 400 to 800 nm, there is a maximum absorption wavelength λmax in a wavelength region of 670 nm or more. ?The following relational expression is established between a maximum absorption constant εA with respect to light with a wavelength of 430 to 550 nm and a maximum absorption constant εB with respect to light with a wavelength of 670 nm or more, where εB/εA≥65. ?In a spectral transmittance curve, an average transmittance of light with a wavelength of 430 to 460 nm is 94.0% or more when a transmittance at the maximum absorption wavelength λmax is set to 1%.
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Paragraph 0314-0316
(2019/01/04)
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- VIRAL REPLICATION INHIBITORS
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The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.
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Page/Page column 186; 187
(2013/04/13)
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- 1,7-Annulated indolocarbazoles as cyclin-dependent kinase inhibitors
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The synthesis and kinase inhibitory activity of a series of novel 1,7-annulated indolocarbazoles 6 and 16 is described. These compounds exhibited potent inhibitory activity against cyclin-dependent kinase 4 and good antiproliferative activity in a human colon carcinoma cell line.
- Al-Awar, Rima S.,Ray, James E.,Hecker, Kyle A.,Huang, Jianping,Waid, Philip P.,Shih, Chuan,Brooks, Harold B.,Spencer, Charles D.,Watkins, Scott A.,Patel, Bharvin R.,Stamm, Nancy B.,Ogg, Catherine A.,Schultz, Richard M.,Considine, Eileen L.,Faul, Margaret M.,Sullivan, Kevin A.,Kolis, Stanley P.,Grutsch, John L.,Joseph, Sajan
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p. 3217 - 3220
(2007/10/03)
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- HETEROCYCLIC COMPOUNDS, METHODS OF MAKING THEM AND THEIR USE IN THERAPY
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In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.
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Page 46-47; 93
(2010/02/07)
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- SEROTONERBIC TETRAHYDROPYRIDOINDOLES
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This invention provides novel, optionally substituted tetrahydropyridoindoles which are useful serotonergic agents for the treatment of central nervous system disorders.
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- Aliphatic carboxamides
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This invention provides a series of novel heterocyclic aliphatic carboxamides of formula I in which the group >Z--Y--XC=CH--NN--CH=CC=N--NN--N=C and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.
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- The Chemistry of Indoles. XXXII. A Facile Synthetic Method for 6-Indolecarbaldehyde, 6-Indolemethanol, and 6-Substituted 1-Hydroxyindoles and Its Application for the Synthesis of a Natural Alkaloid, (E)-6-(3-Methylbuta-1,3-dienyl)indole
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Trivalent titanium ion can reduce arylaldehydes, and the reaction is controllable by selecting the pH of the reaction medium.Utilizing this new finding, 6-indolecarbaldehyde and 6-indolemethanol were conveniently produced by the modified Leimgruber-Batcho method with titanium(III) chloride as the reducing agent.Syntheses of a natural alkaloid, (E)-6-(3-methylbuta-1,3-dienyl)indole, and some new 6-substituted 1-hydroxyindoles are also reported.Keywords-titanium(III) chloride; 6-indolecarbaldehyde; 6-indolemethanol; (E)-6-(3-methylbuta-1,3-dienyl)indole; (Z)-6-(3-methylbuta-1,3-dienyl)indole; 1-hydroxy-6-indolecarbaldehyde; 1-methoxy-6-indolecerbaldehyde; 1-acetoxy-6-indolecarbaldehyde; Leimgruber-Batcho method; reduction
- Somei, Masanori
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p. 4109 - 4115
(2007/10/02)
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