Novel 5beta-hydroxyspirostan-6-ones ecdysteroid antagonists: synthesis and biological testing.
Autor(es): Rivera Daniel G; León Fredy; Coll Francisco; Davison Gema P
Resumo: 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.
Palavras-Chave: Steroids; Antiecdysteroid activity; Spirostanones; Steroidal sapogenins
Imprenta: Steroids, v. 71, n. 1, p. 1-11, 2006
Identificador do objeto digital: 10.1016/j.steroids.2005.02.024
Descritores: Aedes aegypti - Molecular Structure
Data de publicação: 2006
