211805-65-1Relevant academic research and scientific papers
Synthesis of indanones via solid-supported [2+2+2] cyclotrimerization
Senaiar, Ramesh S.,Teske, Jesse A.,Young, Douglas D.,Deiters, Alexander
, p. 7801 - 7804 (2008/03/11)
(Chemical Equation Presented) A new facile approach toward natural and unnatural indanones has been developed, featuring a solid-supported [2+2+2] cyclotrimerization as the key step. This strategy has been applied to the chemo- and regioselective assembly of indanone arrays and to the total synthesis of a recently isolated indanone marine natural product.
Novel imidazolyl and triazolyl substituted biphenyl compounds: Synthesis and evaluation as nonsteroidal inhibitors of human 17α-Hydroxylase-C17, 20-lyase (P450 17)
Zhuang, Yan,Wachall, Bertil G.,Hartmann, Rolf W.
, p. 1245 - 1252 (2007/10/03)
The synthesis of a new series of P450 17 inhibitors is described. The imidazol-1-yl compounds 5 showed strong inhibition of P450 17 rat and especially human enzyme, the most active compounds being 5ax, 5ay and 5bx with IC50 values of 0.17, 0.24 and 0.25 μM, respectively (ketoconazole: 0.74 μM). The 1,2,4-triazol-1-yl compounds 6 were less active, while the 1,2,4-triazol-4-yl compounds 7 were inactive. The title compounds showed little inhibition of P450 arom. The most active P450 17 inhibitors 5ax and 5ay markedly decreased the testosterone plasma concentration of SD rats 2 h after application of 0.019 mmol/kg. After 6 h, 5ay still exhibited a strong effect. Copyright (C) 2000 Elsevier Science Ltd.
