Bicyclic melatonin receptor agonists containing a ring-junction nitrogen: Synthesis, biological evaluation, and molecular modeling of the putative bioactive …

…, F Boeckler, K Davidson, D Sugden, P Gmeiner

文献索引：Elsner, Jan; Boeckler, Frank; Davidson, Kathryn; Sugden, David; Gmeiner, Peter Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 6 p. 1949 - 1958

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被引用次数: 33

摘要

Employing 1, 3-dipolar cycloaddition for the synthesis of the 7a-azaindole nucleus, analogues of melatonin have been synthesized and tested against human and amphibian melatonin receptors. Introducing a phenyl substituent in position 2 of the heterocyclic moiety significantly increased binding affinity to both the MT1 and MT2 receptors. Shifting the methoxy group from position 5 to 2 of the 7a-azaindole ring led to a substantial reduction ...