- Acrylamide derivative and preparation method and application thereof
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The invention belongs to the field of chemical medicines, and particularly relates to an acrylamide derivative. The acrylamide derivative adopts a structural general formula as follows: FORMULA. Someembodiments of the acrylamide derivative confirm that th
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Paragraph 0026; 0028; 0030
(2018/07/30)
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- Synthesis of 12-hetaryl-9,9-dimethyl-7,8,9,10-tetrahydrobenzo[a]acridin- 11(12H)-ones
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Three-component condensation of naphthalen-2-amine with 5-arylfuran(thiophene, N-methylpyrrole)-2-carbaldehyde and 5,5- dimethylcyclohexane-1,3-dione, as well as condensation of N-[(5- arylfuran(thiophen)-2-ylmethylidene]naphthalen-2-amine with 5,5- dimethylcyclohexane-1,3-dione gave the corresponding 12-[5-arylfuran(thiophen, N-methylpyrrol)-2-yl]-7,8,9,10-tetradrobenzo[a]acridin-11(12H)-ones.
- Kozlov,Zhikharko,Lytvyn,Gorak,Skakovskii,Baranovskii,Basalaeva,Obushak
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p. 833 - 839
(2014/08/18)
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- Discovery of new Gram-negative antivirulence drugs: Structure and properties of novel E. coli WaaC inhibitors
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Heptosyltransferases such as WaaC represent promising and attractive targets for the discovery of new Gram-negative antibacterial drugs based on antivirulence mechanisms. We report herein our approach to the identification of the first micromolar inhibitors of WaaC and the preliminary SAR generated from this family of 2-aryl-5-methyl-4-(5-aryl-furan-2-yl-methylene)-2,4-dihydro-pyrazol-3-on es identified by virtual screening.
- Moreau,Desroy,Genevard,Vongsouthi,Gerusz,Le Fralliec,Oliveira,Floquet,Denis,Escaich,Wolf,Busemann,Aschenbrenner
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scheme or table
p. 4022 - 4026
(2009/04/06)
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- Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid
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A novel series of nonnucleoside HCV NS5B polymerase inhibitors were prepared from (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid, a high throughput screening lead. SAR studies combined with structure based drug design focusing on the southern heterobiaryl region of the template led to the synthesis of several potent and orally bioavailable lead compounds. X-ray crystallography studies were also performed to understand the interaction of these inhibitors with HCV NS5B polymerase.
- Pfefferkorn, Jeffrey A.,Greene, Meredith L.,Nugent, Richard A.,Gross, Rebecca J.,Mitchell, Mark A.,Finzel, Barry C.,Harris, Melissa S.,Wells, Peter A.,Shelly, John A.,Anstadt, Robert A.,Kilkuskie, Robert E.,Kopta, Laurice A.,Schwende, Francis J.
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p. 2481 - 2486
(2007/10/03)
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- Structure-activity relationships of novel anti-malarial agents. Part 7: N-(3-benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-furyl)acrylic acid amides with polar moieties
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In a previous report, we have provided evidence that novel anti-malarial compounds based on 2,5-diaminobenzophenone farnesyltransferase inhibitors might benefit from the presence of a polar moiety at the para position of the terminal phenyl of the arylfur
- Wiesner, Jochen,Mitsch, Andreas,Jomaa, Hassan,Schlitzer, Martin
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p. 2159 - 2161
(2007/10/03)
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