Synthesis of novel capital EM, Cyrilliccapital TE, Cyrillic3 receptor ligands via an unusual Knoevenagel condensation.

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Volkova MS, Jensen KC, Lozinskaya NA, Sosonyuk SE, Proskurnina MV, Mesecar AD, Zefirov NS

Synthesis of novel capital EM, Cyrilliccapital TE, Cyrillic3 receptor ligands via an unusual Knoevenagel condensation.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7578-81. doi: 10.1016/j.bmcl.2012.10.005. Epub 2012 Oct 17.

PubMed ID

23131339 [ View in PubMed

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Abstract

New 5-acetamido-substituted melatonin derivatives were efficiently synthesized in excellent yields via Knoevenagel condensation. The relative binding affinity of new synthesized compounds to MT3 receptor was tested via enzymatic assays and the X-ray structures of the most potent compounds were determined in complex with MT3.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Melatonin	Ribosyldihydronicotinamide dehydrogenase [quinone]	IC 50 (nM)	6600	N/A	N/A	Details
Melatonin	Ribosyldihydronicotinamide dehydrogenase [quinone]	IC 50 (nM)	11300	N/A	N/A	Details