SYNTHESIS AND EVALUATION OF THE ANTI-OVULATORY ACTIVITY OF A VARIETY OF MELATONIN ANALOGS

A series of melatonin analogues was synthesized and examined for ovulation-blocking activity. 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 α-methylene; however, a pronounced enhancement resulted from halogenation of the 6 position. © 1979, American Chemical Society. All rights reserved.