Evaluation of piperidinoethoxy moiety as an antiestrogenic substituent in non-steroidal anti-estrogens: Fertility regulation

A piperidinoethoxy substituent in non-steroidal antiestrogens has a relatively higher antiestrogenic effects as compared to a pyrrolidinoethoxy moiety. However, the antagonistic activity is more depended on the molecular geometry than the nature of the basic chain. No significant difference in the a...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 7; no. 16; pp. 2131 - 2136
Main Authors Tripathi, Sachi, Dwivedy, Indra, Dhar, J.D, Dwivedy, Anila, Ray, Suprabhat
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 19.08.1997
Elsevier
Subjects
Biological and medical sciences
Genital system. Reproduction
Medical sciences
Pharmacology. Drug treatments
Rat
Nitrogen heterocycle
Rodentia
Antiestrogen
Estrogen
Aminoether
Female sterility
Antihormone
Oxygen heterocycle
Modeling
Pyrrolidine derivatives
Chroman derivatives
Vertebrata
Biological fixation
Mammalia
Structure activity relation
Animal
Molecular model
Piperidine derivatives
Bicyclic compound
Contraceptive
Chemical synthesis
Non steroid compound
Hormonal receptor
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Summary:A piperidinoethoxy substituent in non-steroidal antiestrogens has a relatively higher antiestrogenic effects as compared to a pyrrolidinoethoxy moiety. However, the antagonistic activity is more depended on the molecular geometry than the nature of the basic chain. No significant difference in the antifertility activity in these two sets of compounds was observed. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)00379-X