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Application of the bridgehead fragments for the design of conformationally restricted melatonin analogues.
- Source :
-
Bioorganic chemistry [Bioorg Chem] 2011 Apr; Vol. 39 (2), pp. 67-72. - Publication Year :
- 2011
-
Abstract
- Conformationally constrained analogues of the hormone melatonin with a side chain incorporated into the bicyclic bridgehead core were synthesized based on the homology modeling and molecular docking studies performed for the MT(2) melatonin receptor. The methoxy-indole derivative fused with exo-N-acetamino-substituted bicyclo[2.2.2]octane was found to possess nanomolar MT(2) receptor affinity.<br /> (Copyright © 2011 Elsevier Inc. All rights reserved.)
- Subjects :
- Bridged Bicyclo Compounds chemistry
Computer Simulation
Indoles chemistry
Melatonin chemical synthesis
Molecular Conformation
Receptor, Melatonin, MT1 chemistry
Receptor, Melatonin, MT1 metabolism
Receptor, Melatonin, MT2 chemistry
Receptor, Melatonin, MT2 metabolism
Melatonin analogs & derivatives
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2120
- Volume :
- 39
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 21419469
- Full Text :
- https://doi.org/10.1016/j.bioorg.2011.02.002