Synthesis and evaluation of the antiovulatory activity of a variety of melatonin analogs

Abstract

A series of melatonin analogus was synthesized and examined for ovulation-blocking activity in rats. Deviation from the 5-methoxy group or substitution of the 1 position prevented activity. Activity was not particularly sensitive to minor variations in the N-acyl group nor was it significantly altered by methylation of position 2 or the .alpha.-methylene; however, a pronounced enhancement resulted from halogenation of the 6 position.