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Chemical Compound Review:

PubChem20200 1H-indole-2-carboxamide

Synonyms: SureCN118686, AG-E-16460, ALBB-007757, AK-47015, KB-12399, ...

Cooper, S.J. et al., Nagy, J., Ragno, R. et al., Wright, C.D. et al., De Martino, G. et al., et al.

Ragno, Coluccia, La Regina, De Martino, Piscitelli, Lavecchia, Novellino, Bergamini, Ciaprini, Sinistro, Maga, Crespan, Artico, Silvestri, Borza, Kolok, Gere, Agai-Csongor, Agai, Tárkányi, Horváth, Barta-Szalai, Bozó, Kiss, Bielik, Nagy, Farkas, Domány, Nagy,

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Disease relevance of Indole, 2-carboxamide-

Indolyl aryl sulphones as HIV-1 non-nucleoside reverse transcriptase inhibitors: synthesis, biological evaluation and binding mode studies of new derivatives at indole-2-carboxamide [1].

High impact information on Indole, 2-carboxamide-

Molecular modeling studies and an updated highly predictive 3-D QSAR model led to the discovery of exceptionally potent indolyl aryl sulfones (IASs) characterized by the presence of either a pyrrolidyn-2-one nucleus at the indole-2-carboxamide or some substituents at the indole-2-carbohydrazide [2].
Novel indole-2-carboxamide and cycloalkeno[1,2-b]indole derivatives. Structure-activity relationships for high inhibition of human LDL peroxidation [3].
1. Experiments were conducted to determine whether or not the effect of (+)-fenfluramine (3.0 mg kg-1, i.p.) on food intake can be antagonized by the selective cholecystokinin receptor antagonist MK-239 (formerly L364,718; (3S(-)-N-(2,3-dihydro-1-methyl-2-oxo-5-phenyl-1-H-1,4-benzodiazepin++ +-3-yl)-1H- indole-2-carboxamide) [4].
CI-949 [5-methyl-3-(1-methylethoxy)-1-phenyl-N-1H-tetrazol-5-yl-1H- indole-2- carboxamide, L-arginine salt] inhibits human neutrophil activation in response to stimuli which promote calcium mobilization or calcium influx [5].
A novel series of indole-2-carboxamide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists [6].

Biological context of Indole, 2-carboxamide-

Recently emerged NR2B SSNAs (CP-101606 (Pfizer Inc), Co-101244 (Pfizer Inc/Purdue Neuroscience Corp/Senju Pharmaceutical Co Ltd), CI-1041 (Purdue Neuroscience Corp/Pfizer Inc) and indole-2-carboxamide derivatives) have demonstrated excellent in vitro potency against withdrawal-induced cytotoxicity [7].

References

Indolyl aryl sulphones as HIV-1 non-nucleoside reverse transcriptase inhibitors: synthesis, biological evaluation and binding mode studies of new derivatives at indole-2-carboxamide. De Martino, G., La Regina, G., Ragno, R., Coluccia, A., Bergamini, A., Ciaprini, C., Sinistro, A., Maga, G., Crespan, E., Artico, M., Silvestri, R. Antivir. Chem. Chemother. (2006) [Pubmed]
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide. Ragno, R., Coluccia, A., La Regina, G., De Martino, G., Piscitelli, F., Lavecchia, A., Novellino, E., Bergamini, A., Ciaprini, C., Sinistro, A., Maga, G., Crespan, E., Artico, M., Silvestri, R. J. Med. Chem. (2006) [Pubmed]
Novel indole-2-carboxamide and cycloalkeno[1,2-b]indole derivatives. Structure-activity relationships for high inhibition of human LDL peroxidation. Kuehm-Caubere, C., Caubere, P., Jamart-Gregoire, B., Negre-Salvayre, A., Bonnefont-Rousselot, D., Bizot-Espiard, J.G., Pfeiffer, B., Caignard, D.H., Guardiola-Lemaitre, B., Renard, P. J. Med. Chem. (1997) [Pubmed]
Reversal of the anorectic effect of (+)-fenfluramine in the rat by the selective cholecystokinin receptor antagonist MK-329. Cooper, S.J., Dourish, C.T., Barber, D.J. Br. J. Pharmacol. (1990) [Pubmed]
Inhibition of human neutrophil activation by the allergic mediator release inhibitor, CI-949: mechanism of inhibitory activity. Wright, C.D., Kuipers, P.J., Hoffman, M.D., Thueson, D.O., Conroy, M.C. Biochem. Biophys. Res. Commun. (1990) [Pubmed]
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists. Borza, I., Kolok, S., Gere, A., Agai-Csongor, E., Agai, B., Tárkányi, G., Horváth, C., Barta-Szalai, G., Bozó, E., Kiss, C., Bielik, A., Nagy, J., Farkas, S., Domány, G. Bioorg. Med. Chem. Lett. (2003) [Pubmed]
Renaissance of NMDA receptor antagonists: do they have a role in the pharmacotherapy for alcoholism? Nagy, J. IDrugs : the investigational drugs journal. (2004) [Pubmed]

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