Steroid antifertility agents. Ionic complexes of basic derivatives for prolonged action.

A P Gray; T N Yamauchi

doi:10.1021/jm00205a027

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Steroid antifertility agents. Ionic complexes of basic derivatives for prolonged action.

A P Gray·T N Yamauchi

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Abstract

Ethynylestradiol 3-dimethylaminopropionate (1), norethindrone 3-(O-dimethylaminopropyl)oxime (syn and anti isomers, 2a and 2b), and testosterone 3-(O-dimethylaminopropyl)oxime (3) have been prepared and converted to zinc and aluminum tannate complexes as potentially long-acting prodrug forms of the parent steroids. The basic derivatives and the complexes showed the appropriate hormonal activities although they were less active in acute tests than the respective parents. The complexes of 1 showed prolonged activities and, in particular, the zinc tannate showed a prolonged duration of antifertility activity in the rat on subcutaneous administration in an aluminum monostearate gel.

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Animals Contraceptive Agents Delayed-Action Preparations Ethinyl Estradiol Female Fertility Injections, Subcutaneous Norethindrone Organ Size Rabbits Rats Testosterone Time Factors Uterus Journal Article Research Support, U.S. Gov't, P.H.S.

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A P Gray, T N Yamauchi. 1978. Steroid antifertility agents. Ionic complexes of basic derivatives for prolonged action.. https://doi.org/10.1021/jm00205a027

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