- The Chemistry of Ethyl 3-(2-Ethoxy-2-oxoethyl)-1 H -indole-2-carboxylate: Synthesis of Pyrimido[4,5- b ]indoles and Diethyl 4-Hydroxyquinoline-2,3-dicarboxylate via Intramolecular Cyclizations
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We report the synthesis of a new series of 2-oxo-1,2,4,9-tetrahydro-3H-pyrimido[4,5-b]indole derivatives and diethyl 4-hydroxyquinoline-2,3-dicarboxylate starting from ethyl 3-(2-ethoxy-2-oxoethyl)-1H-indole-2-carboxylate. Intramolecular cyclization forme
- Kapti, Tolga,Dengiz, Cagatay,Balci, Metin
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p. 1898 - 1904
(2017/04/06)
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- Indole- and indoline-based kainate analogues with antagonist activity at ionotropic glutamate receptors
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A conformationally constrained, indole-based kainate analogue was designed based on Gouaux's X-ray structure of kainic acid bound to an iGluR2(S1S2) construct, a structural model for AMPA/kainate ionotropic glutamate receptors. In contrast to the parent kainic acid, a potent agonist, this compound, along with three structurally related analogues derived from synthetic intermediates, exhibited antagonist behavior towards KAR expressed in oocytes, a result that is rationalized by molecular modeling studies.
- Shou, Xiaohong,Miledi, Ricardo,Chamberlin, A. Richard
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p. 3942 - 3947
(2007/10/03)
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- Regiospecific functionalization of indole-2-carboxylates and diastereoselective preparation of the corresponding indolines
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The N-acyl derivatives of 3-substituted indole-2-carboxylates prepared through several routes were submitted to catalytic hydrogenation affording either cis- or trans-indoline diastereomers after quantitative C-2 epimerization.
- Collot, Valerie,Schmitt, Martine,Marwah, Padma,Bourguignon, Jean-Jacques
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p. 2823 - 2847
(2007/10/03)
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- Compositions containing indole-2-carboxylate compounds for treatment of CNS disorders
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Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders
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- Novel Indole-2-carboxylates as Ligands for the Strychnine-Insensitive N-Methyl-D-aspartate-Linked Glycine Receptor
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A series of indole-2-carboxylates were prepared and evaluated for their ability to inhibit the binding at the strychnine-insensitive glycine receptor that is associated with the NMDA-PCP-glycine receptor complex.All of the compounds were selective for the glycine site relative to other sites on the receptor macrocomplex and several of the compounds in this series were found to have submicromolar affinity for this receptor.The lead compound, 2-carboxy-6-chloro-3-indoleacetic acid (Ki = 1.6 μM vsglycine), was also found to noncompetitively inhibit the binding of MK-801, a ligand for the phencyclidine site on the receptor macrocomplex.These latter data suggest that the compound functions as an antagonist at the strychnine-insensitive glycine receptor.The structural activity relationships within this series of indole-2-carboxylates is discussed and several key pharmacophores are identified for this series of glycine ligands.In general, the most potent compounds were the C-3 acetamides, with N-propyl-2-carboxy-6-chloro-3-indoleacetamide having the highest receptor affinity.
- Gray, Nancy M.,Dappen, Michael S.,Cheng, Brian K.,Cordi, Alexis A.,Biesterfeldt, John P.,et al.
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p. 1283 - 1292
(2007/10/02)
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- A convenient Synthesis of New Indole Derivatives
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Several indole derivatives (IIa-g) have been prepared by refluxing equimolar amounts of the appropriate indole and 2,4-dinitrobenzoyl chloride, p-bromoaniline, isobutyl chloroformate and N-bromosuccinimide in ethanol in the presence of sodium acetate.
- Saleha, Sabiha,Siddiqui, Amin A.,Khan, Nassem H.
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