197243-46-2Relevant academic research and scientific papers
Overcoming AlbD Protease Resistance and Improving Potency: Synthesis and Bioactivity of Antibacterial Albicidin Analogues with Amide Bond Isosteres
Kleebauer, Leonardo,Zborovsky, Lieby,Hommernick, Kay,Seidel, Maria,Weston, John B.,Süssmuth, Roderich D.
supporting information, p. 7023 - 7027 (2021/09/08)
Albicidin is a potent antibacterial oligoaromatic peptide that is susceptible to the protease AlbD, a resistance factor. This potentially restricts the use of albicidin as a drug. To overcome this obstacle, we synthesized and evaluated six analogues with
FUSED RING COMPOUND HAVING UREA STRUCTURE
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Page/Page column 230, (2020/01/31)
The present invention relates to a novel fused ring compound having urea structure that exhibits excellent NAMPT activating effect, and a method using the same for treating / preventing metabolic disorder, cardiovascular and kidney disease, mitochondrial disease, neurodegenerative disease, ocular disease, and muscle wasting disorder. The present invention provides a compound represented by following formula (I) or a pharmacologically acceptable salt: Formula (I) wherein A, B, R, R2 and R3 represent the same meanings as in the claims.
Macrocyclic Modulators of the Ghrelin Receptor
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Paragraph 0474, (2018/05/03)
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Method for synthesizing asymmetric C-O coupled compound and application of asymmetric C-O coupled compound
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Paragraph 0114; 0115, (2016/10/07)
The invention discloses a method for synthesizing an asymmetric C-O coupled compound and application of the asymmetric C-O coupled compound and belongs to the technical field of chemical synthesis. According to the method, a compound represented by a form
FUNCTIONALISED AND SUBSTITUTED INDOLES AS ANTI-CANCER AGENTS
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Page/Page column 124, (2016/12/22)
The present invention relates broadly to functionalised and substituted indoles, the preparation thereof and their use in the treatment of proliferative diseases such as cancer.
A quantitative structure-reactivity assessment of phenols by investigation of rapid iodination kinetics using hydrodynamic voltammetry: Applicability of the Hammett equation in aqueous medium
Borkar, Vitthal T.,Bonde, Shantaram L.,Dangat, Vijay T.
, p. 693 - 702 (2013/10/21)
Halogenations of aromatic substrates in aqueous medium are essentially electrophilic substitutions proceeding at rates concomitant with the nature of the substrates and substituent motifs. Kinetics as an investigatory tool for the quantitative assessment of the structure-reactivity correlation in these reactions for a diverse range of substrates has rarely been reported, presumably due to the rapidity of these reactions in aqueous medium. We have used hydrodynamic voltammetry to investigate the rapid kinetics of uncatalyzed iodination of phenol and eight substituted phenols by iodine monochloride at constant pH in aqueous medium. The Arrhenius plots for these reactions yield comprehensive kinetic and thermodynamic data. The quantitative structure-reactivity correlation stemming from the regio- and stereospecificity of the substituent motifs on the substrates has been examined through the Hammett plot, which shows a negative slope of 1.87. The magnitudes of the rate constants, energies of activation, frequency factors, and entropy change obtained for the nine fast reactions reported, reflect the relative ease of the reaction dynamics in quantitative terms thereby ascertaining the relative reactivities of the phenols studied herein.
5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS AS UROTENSIN II RECEPTOR ANTAGONISTS
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Page/Page column 23, (2009/12/28)
The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.
Chemistry of aminophenols. Part 3: First synthesis of nitrobenzo[b]furans via a coupling-cyclization approach
Dai, Wei-Min,Lai, Kwong Wah
, p. 9377 - 9380 (2007/10/03)
The first synthesis of 4-, 5-, and 6-nitrobenzo[b]furans has been achieved via the Sonogashira cross-coupling reaction of 2-iodonitrophenol acetates prepared from commercially available and inexpensive 2-aminonitrophenols. The obtained 2-alkynylnitropheno
Iodination of Thallium(I) salts of Phenols
Gambie, Richard C.,Larsen, David S.,Rutledge, Peter S.,Woodgate, Paul D.
, p. 767 - 769 (2007/10/03)
The iodination of thallium(I) salts of phenols is examined and the results are compared with those of the selective ortho-iodinating reagent thallium(I) acetate-iodine.
