Novel 5beta-hydroxyspirostan-6-ones ecdysteroid antagonists: synthesis and biological testing |
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Authors: | Rivera Daniel G León Fredy Coll Francisco Davison Gema P |
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Affiliation: | Center for Natural Products Studies, Faculty of Chemistry, University of Havana, Zapata y G, Vedado 10400, Ciudad Habana, Cuba. drivera@ipb-halle.de |
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Abstract: | Eight new 5beta-hydroxy-spirostan-6-ones bearing hydroxy and amino functions in the A ring, i.e., 3beta-OH, 3alpha-OH, 2beta,3beta-OH, 2alpha,3beta-OH, 3beta-NH2, 2alpha-NH2-3beta-OH, 2beta-NH2-3beta-OH, and 2beta-OH-3beta-NH2, were efficiently synthesized, and their antiecdysteroid activities were evaluated on the metamorphosis bioassay of mosquito Aedes aegypti. To our knowledge, these new steroids represent the first 5beta-hydroxy-spirostanes which have been tested for antiecdysteroid activity in mosquitoes. The higher antagonistic effect was found for compounds bearing the 3beta-hydroxy and 2beta,3beta-dihydroxy functionality, which show promise as environmental friendly insecticides. |
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Keywords: | Steroids Antiecdysteroid activity Spirostanones Steroidal sapogenins |
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