Substituted 2-Amidomethyl[1,4]benzodioxins: Synthesis and Binding Affinity for the Melatonin Receptors

A novel series of melatonin analogues based on the benzodioxin nucleus is described. The compounds were prepared in several steps from 2‐carbethoxy‐1,4‐benzodioxin. Some of these derivatives competitively inhibited 2‐[125I]‐iodomelatonin binding to chicken brain and ovine pars tuberalis membranes, a...

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Bibliographic Details
Published in:Pharmacy and Pharmacology Communications 1999-03, Vol.5 (3), p.199-206
Main Authors: MAMAI, A., BENNEJEAN, C., RENARD, P., DELAGRANGE, P., GUARDIOLA-LEMAITRE, B., HOWELL, H. E., VIAUD, M. C., GUILLAUMET, G.
Format: Article
Language:English
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Summary:A novel series of melatonin analogues based on the benzodioxin nucleus is described. The compounds were prepared in several steps from 2‐carbethoxy‐1,4‐benzodioxin. Some of these derivatives competitively inhibited 2‐[125I]‐iodomelatonin binding to chicken brain and ovine pars tuberalis membranes, albeit with very reduced affinity compared with melatonin.
ISSN:1460-8081
2042-7158
DOI:10.1211/146080899128734604