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Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2015 Mar 15; Vol. 23 (6), pp. 1313-20. Date of Electronic Publication: 2015 Jan 24. - Publication Year :
- 2015
-
Abstract
- A novel series of 4-nitroindole sulfonamides containing a methyleneamino-N,N-dimethylformamidine were prepared. The binding of these compounds to 5-HT2A and 5-HT2C was evaluated, and most of the compounds showed IC50 values of less than 1μM, and exhibited high selectivity for the 5-HT2C receptor. However, little selectivity was observed in the functional assay for 5-HT6 receptors. The computational modeling studies further validated the biological results and also demonstrated a reasonable correlation between the activity of compounds and the mode of superimposition with specified pharmacophoric features.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Dose-Response Relationship, Drug
Humans
Indoles chemical synthesis
Indoles chemistry
Molecular Structure
Nitro Compounds chemical synthesis
Nitro Compounds chemistry
Recombinant Proteins metabolism
Serotonin 5-HT2 Receptor Antagonists chemistry
Structure-Activity Relationship
Indoles pharmacology
Nitro Compounds pharmacology
Receptor, Serotonin, 5-HT2A metabolism
Serotonin 5-HT2 Receptor Antagonists chemical synthesis
Serotonin 5-HT2 Receptor Antagonists pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 23
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 25684421
- Full Text :
- https://doi.org/10.1016/j.bmc.2015.01.032