- TRICYCLIC FURAN-SUBSTITUTED PIPERIDINEDIONE COMPOUND
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Disclosed are a series of tricyclic furan-substituted piperidinedione compounds and an application thereof in preparing a drug for treating a disease related to CRBN protein. In particular, disclosed is a derivative compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
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Paragraph 0155; 0157
(2021/07/17)
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- FUNCTIONALIZED HETEROCYCLES AS ANTIVIRAL AGENTS
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The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
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- Synthesis and preliminary evaluation of benzofuran-oxadiazole conjugates as potential antitubercular agents
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In the present study, a series of benzofuran-oxadiazole conjugates 7(a-o) was designed, synthesized and characterized through IR,1H NMR,13C NMR and mass spectral data. All the compounds were screened for preliminary antitubercular activity against Mycobacterium phlei and Mycobacterium tuberculosis H37RV. Among all the target compounds, the compound possessing chlorine (7k, MIC 1.56 μg/mL) and bromine (7m, MIC 1.56 μg/mL) on 6th position of benzofuran showed highest activity against Mycobacterium phlei. Whereas, bromine on either 5th position (7l, MIC 3.125 μg/mL) or 6th position (7m MIC 3.125 μg/mL) on benzofuran exhibited highest activity for Mycobacterium tuberculosis (H37 RV).
- Negalurmath, Veerabhadrayya S.,Kotresh, Obelannavar,Basanagouda, Mahantesha
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p. 965 - 970
(2019/03/07)
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- Design and synthesis of tailored human caseinolytic protease P inhibitors
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Human caseinolytic protease P (hClpP) is important for degradation of misfolded proteins in the mitochondrial unfolded protein response. We here introduce tailored hClpP inhibitors that utilize a steric discrimination in their core naphthofuran scaffold to selectively address the human enzyme. This novel inhibitor generation exhibited superior activity compared to previously introduced beta-lactones, optimized for bacterial ClpP. Further insights into the bioactivity and binding to cellular targets were obtained via chemical proteomics as well as proliferation- and migration studies in cancer cells.
- Gronauer, Thomas F.,Mandl, Melanie M.,Lakemeyer, Markus,Hackl, Mathias W.,Me?ner, Martina,Korotkov, Vadim S.,Pachmayr, Johanna,Sieber, Stephan A.
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supporting information
p. 9833 - 9836
(2018/09/10)
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- Efficient and Convenient Method for Synthesis of Benzofuran-3-acetic Acids and Naphthafuran-acetic Acids
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Herein, we report an efficient and convenient method for synthesis of benzofuran-3-acetic acids and naphthafuran-acetic acids 5a-p by the reaction of substituted-4-bromomethylcoumarins with aqueous sodium hydroxide at refluxing temperature. The obtained products are characterized by infrared, 1H NMR, 13C NMR, and mass spectral data. Structures 5a and 5e are confirmed by their single x-ray diffraction studies. The advantages of this method are good yields, easy workup, and no chromatographic purifications.
- Basanagouda, Mahantesha,Narayanachar,Majati, Iranna B.,Mulimani, Shiddappa S.,Sunnal, Satish B.,Nadiger, Rohit V.,Ghanti, Ashok S.,Gudageri, Siddeshwar F.,Naik, Ravi,Nayak, Akshata
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supporting information
p. 2195 - 2202
(2015/09/22)
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- Preparation of (2,3-dihydrobenzofuran-3-yl)acetic acid via Rh-catalyzed asymmetric hydrogenation
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A preparation via Rh-catalyzed asymmetric hydrogenation has been developed for (2,3-dihydrobenzofuran-3-yl)-acetic acid derivatives, a key intermediate in the synthesis of the active pharmaceutical ingredient for GPR40 agonist, fasiglifam. Use of a cationic rhodium-Et-FerroTANE complex yielded the desired product in high enantiomeric excess (91%) and quantitative yield, and was thus recommended for further process development.
- Yamashita, Masayuki,Negoro, Nobuyuki,Yasuma, Tsuneo,Yamano, Toru
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p. 539 - 543
(2014/05/06)
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- Carboxylic fused furans for amino acid fluorescent labelling
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Four carboxylic fused furans are presented as new fluorescent labels for the amino and hydroxyl functions of organic molecules. Various representative l-amino acids were chosen as models, labelled at their N-terminus and also at their side-chain. Fluoresc
- Piloto, Ana M.,Fonseca, Andrea S.C.,Costa, Susana P.G.,Gon?alves, M. Sameiro T.
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p. 9258 - 9267
(2007/10/03)
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- FUNGICIDAL HETEROCYCLIC COMPOUNDS
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A compound which can specifically or selectively expresses an antifungal activity with a broad spectrum, based on the functional mechanism of 1,6-β-glucan synthesis inhibition, is provided, and an antifungal agent which comprises such a compound, a salt thereof or a solvate thereof is provided. A compound represented by the following formula (I), a salt thereof or a solvate thereof.
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Page/Page column 52
(2010/11/24)
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