V. Leclerc et al., SYNTHESIS AND BIOLOGICAL-ACTIVITY OF CONFORMATIONALLY RESTRICTED TRICYCLIC ANALOGS OF THE HORMONE MELATONIN, Bioorganic & medicinal chemistry letters, 6(10), 1996, pp. 1071-1076
A serie of rotationally restricted tricyclic naphthalenic and tetrahyd
ronaphthalenic analogs of the hormone melatonin has been synthesized,
the C-7 oxygen being incorporated in a pyran, furan or dioxan heterocy
clic ring. The receptor binding profile of these compounds is a functi
on of the directionality of the lone pairs electrons of this C-7 oxyge
n. In these two studied analogous series the agonist activity seems to
be correlated with the existence of a naphthalene nucleus. (C) 1996 E
lsevier Science Ltd