Category: 128717-77-1

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, MedChemComm called Design, synthesis, and structure-activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists, Author is Adam, Julia M.; Cairns, Jim; Caulfield, Wilson; Cowley, Phillip; Cumming, Iain; Easson, Morag; Edwards, Darren; Ferguson, Morag; Goodwin, Richard; Jeremiah, Fiona; Kiyoi, Takao; Mistry, Ashvin; Moir, Elizabeth; Morphy, Richard; Tierney, Jason; York, Mark; Baker, James; Cottney, Jean E.; Houghton, Andrea K.; Westwood, Paul J.; Walker, Glenn, which mentions a compound: 128717-77-1, SMILESS is O=C(C1=CNC2=C1C=CC=C2OC)O, Molecular C10H9NO3, Synthetic Route of C10H9NO3.

A novel CB1 receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded a single confirmed hit with poor water solubility Structural variations were explored with the aim of introducing water solubility and improving potency. This led to the discovery of Org 28611, a potent, water soluble CB1 receptor agonist, which was selected for clin. evaluation as a potential i.v. analgesic agent.

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Pei, Chunzhe; Zong, Jiarui; Han, Shanglin; Li, Bin; Wang, Baiquan published an article about the compound: 7-Methoxy-1H-indole-3-carboxylic acid( cas:128717-77-1,SMILESS:O=C(C1=CNC2=C1C=CC=C2OC)O ).Synthetic Route of C10H9NO3. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:128717-77-1) through the article.

The transition-metal-catalyzed direct carboxylation of an unactivated C-H bond is rarely reported, and no example of catalysis using abundant and cheap nickel has been reported. In this work, the first Ni-catalyzed direct carboxylation of an unactivated C-H bond under an atm. pressure of CO2 is reported. This method affords moderate to high carboxylation yields of various Me carboxylates under mild conditions. Preliminary mechanistic studies reveal that a Ni(0)-Ni(II)-Ni(I) catalytic cycle may be involved in this reaction.

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 128717-77-1, is researched, SMILESS is O=C(C1=CNC2=C1C=CC=C2OC)O, Molecular C10H9NO3Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Development and Profiling of Inverse Agonist Tools for the Neuroprotective Transcription Factor Nurr1, Author is Zaienne, Daniel; Willems, Sabine; Schierle, Simone; Heering, Jan; Merk, Daniel, the main research direction is inverse agonist neuroprotective transcription factor Nurr1.Electric Literature of C10H9NO3.

The ligand-sensing transcription factor nuclear receptor related 1 (Nurr1) evolves as an appealing target to treat neurodegenerative diseases. Despite its therapeutic potential observed in various rodent models, potent modulators for Nurr1 are lacking as pharmacol. tools. Here, we report the structure-activity relationship and systematic optimization of indole-based inverse Nurr1 agonists. Optimized analogs decreased the receptor’s intrinsic transcriptional activity by up to more than 90% and revealed preference for inhibiting Nurr1 monomer activity. In orthogonal cell-free settings, we detected displacement of NCoRs and disruption of the Nurr1 homodimer as mol. modes of action. The inverse Nurr1 agonists reduced the expression of Nurr1-regulated genes in T98G cells, and treatment with an inverse Nurr1 agonist mimicked the effect of Nurr1 silencing on interleukin-6 release from LPS-stimulated human astrocytes. The indole-based inverse Nurr1 agonists valuably extend the toolbox of Nurr1 modulators to further probe the role of Nurr1 in neuroinflammation, cancer, and beyond.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 7-Methoxy-1H-indole-3-carboxylic acid( cas:128717-77-1 ) is researched.Application of 128717-77-1.Cox, Brian; Duffy, James; Zdorichenko, Victor; Bellanger, Corentin; Hurcum, Jessica; Laleu, Benoit; Booker-Milburn, Kevin I.; Elliott, Luke D.; Robertson-Ralph, Michael; Swain, Christopher J.; Bishop, Stephen J.; Hallyburton, Irene; Anderson, Mark published the article 《Escaping from Flatland: Antimalarial Activity of sp3-Rich Bridged Pyrrolidine Derivatives》 about this compound( cas:128717-77-1 ) in ACS Medicinal Chemistry Letters. Keywords: pyrrolidine preparation antimalarial activity. Let’s learn more about this compound (cas:128717-77-1).

Synthetic photochem. to generate novel sp3-rich scaffolds and report the design, synthesis, and biol. testing of a diverse series of amides based on the 1-(amino-methyl)-2-benzyl-2-aza-bicyclo[2.1.1]hexane scaffold was utilized . Preliminary antimalarial screening of the library provided promising compounds with activity in the 1-5μM range with an enhanced hit rate. Further evaluation (solubility, drug metabolism and pharmacokinetics (DMPK), and toxicity) of a selected compound (9) suggested that this series represents an excellent opportunity for further optimization with the framework offering multiple opportunities for the addition of uniquely vectorally positioned extra functionality.

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