534572-70-8Relevant articles and documents
Discovery of novel steroidal histamine H3 receptor antagonists/inverse agonists. Part 2. Versatile steroidal carboxamide derivatives
Ledneczki, István,Némethy, Zsolt,Tapolcsányi, Pál,éles, János,Greiner, István,Gábor, Eszter,Varga, Balázs,Balázs, Ottilia,Román, Viktor,Lévay, Gy?rgy,Mahó, Sándor
supporting information, (2019/09/06)
To further proceed with our previous work, novel steroid-based histamine H3 receptor antagonists were identified and characterized. Using an ‘amine-to-amide’ modification strategy at position 17, in vitro and in vivo potent monoamino steroid derivatives were found during the lead optimization. Usage of the non-basic amide moiety resulted in beneficial effects both in activity and selectivity. The 15α-carboxamido derivative 10 was not only highly active at human and rat H3 receptors, but also showed negligible activity at rat muscarinic receptors. Furthermore, it proved to be considerably stable in human and rat microsomes and showed significant in vivo potency in the pharmacodynamic rat dipsogenia test and in the water-labyrinth cognitive model. Based on all of these considerations, compound 10 was appointed to be a preclinical candidate.
15Alpha-substituted estradiol carboxylic acid esters as locally active estrogens
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Page/Page column 2; 7; sheet 2, (2010/02/08)
The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 15α-estradiol ester compounds is presented which exhibit excellent biologica
Synthesis and evaluation of B-, C-, and D-ring-substituted estradiol carboxylic acid esters as locally active estrogens
Labaree, David C.,Zhang, Jing-Xin,Harris, Heather A.,O'Connor, Craig,Reynolds, Toni Y.,Hochberg, Richard B.
, p. 1886 - 1904 (2007/10/03)
We have synthesized derivatives of estradiol that are structurally modified to serve as "soft" estrogens and act within a geographically limited area of the body; estrogens without systemic action. We have previously shown with 16α-substituted analogues o