- Thiazolidine-2,4-dione-based irreversible allosteric IKK-β kinase inhibitors: Optimization into in vivo active anti-inflammatory agents
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Selective kinase inhibitors development is a cumbersome task because of ATP binding sites similarities across kinases. On contrast, irreversible allosteric covalent inhibition offers opportunity to develop novel selective kinase inhibitors. Previously, we
- Elkamhawy, Ahmed,Kim, Nam youn,Hassan, Ahmed H.E.,Park, Jung-eun,Paik, Sora,Yang, Jeong-Eun,Oh, Kwang-Seok,Lee, Byung Ho,Lee, Mi Young,Shin, Kye Jung,Pae, Ae Nim,Lee, Kyung-Tae,Roh, Eun Joo
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- Synthesis, In Vitro Biological Screening, and In Silico Computational Studies of Some Novel Imidazole-2-thiol Derivatives
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Substituted imidazole analogues 2-((5-acetyl-4-methyl-1-phenyl-1H-imidazole-2-yl)thio)-N-phenylacetamides (3a–3m) have been synthesized from 1-[1-(phenyl)-2-mercapto-4-methyl-1H-imidazol-5-yl]-ethanone (1a–1e) and 2-chloro-N-phenylacetamide (2a–2i) in the
- Daraji, Drashti G.,Patel, Kinjal D.,Patel, Hitesh D.,Rajani, Dhanji P.
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- A highly selective and sensitive fluorescent chemosensor for Fe 3+ in physiological aqueous solution
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A novel fluorescent chemosensor in which two aza-18-crown-6 moieties are linked to a coumarin fluorophore has been synthesized for sensing Fe 3+. The selective fluorescence enhancement was observed upon binding Fe3+ at physiological
- Hua, Jun,Wang, Yan-Guang
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- Antidiabetic compounds
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Compounds for the treatment of hyperglycemia and/or diabetes are provided. The compounds, which inhibit the enzyme dipeptidyl peptidase (DPP-4), are based on the structure where X may be present or absent an may be OH, Ar is an aryl group; and n ranges from 0 to 5.
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Page/Page column 13-14
(2020/06/16)
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- Substituted-3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and Stimulator for Interferon Genes (STING) modulators as cancer immunotherapeutics
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Substituted -3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and related compounds, which are useful as inhibitors of ENPP1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the ENPP1.
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Paragraph 0213
(2020/02/19)
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- Substituted-3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and Stimulator for Interferon Genes (STING) modulators as cancer immunotherapeutics
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Substituted-3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and related compounds, which are useful as inhibitors of ENPP1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the ENPP1.
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Paragraph 0231
(2019/02/13)
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- Exploring DOXP-reductoisomerase binding limits using phosphonated N-aryl and N-heteroarylcarboxamides as DXR inhibitors
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DOXP-reductoisomerase (DXR) is a validated target for the development of antimalarial drugs to address the increase in resistant strains of Plasmodium falciparum. Series of aryl- and heteroarylcarbamoylphosphonic acids, their diethyl esters and disodium salts have been prepared as analogues of the potent DXR inhibitor fosmidomycin. The effects of the carboxamide N-substituents and the length of the methylene linker have been explored using in silico docking studies, saturation transfer difference NMR spectroscopy and enzyme inhibition assays using both EcDXR and PfDXR. These studies indicate an optimal linker length of two methylene units and have confirmed the importance of an additional binding pocket in the PfDXR active site. Insights into the constraints of the PfDXR binding site provide additional scope for the rational design of DXR inhibitors with increased ligand-receptor interactions.
- Bodill, Taryn,Conibear, Anne C.,Mutorwa, Marius K.M.,Goble, Jessica L.,Blatch, Gregory L.,Lobb, Kevin A.,Klein, Rosalyn,Kaye, Perry T.
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p. 4332 - 4341
(2013/07/27)
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- 3-substituted anilines as scaffolds for the construction of glutamine synthetase and DXP-reductoisomerase inhibitors
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Access to a series of truncated ATP analogs, as potential anti-tuberculosis agents, has been explored via alkylation and acylation of 3-aminophenol, whereas chloroacetylation, using chloroacetyl chloride, and subsequent Arbuzov phosphonation of a series of 3-substituted anilines have afforded a series of phosphonate derivatives as potential antimalarial agents.
- Mutorwa, Marius,Salisu, Sheriff,Blatch, Gregory L.,Kenyon, Colin,Kaye, Perry T.
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experimental part
p. 2723 - 2736
(2009/12/09)
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