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Application of the bridgehead fragments for the design of conformationally restricted melatonin analogues.

Authors :
Zefirova ON
Baranova TY
Ivanova AA
Ivanov AA
Zefirov NS
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.)

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