666828-90-6Relevant articles and documents
1-[(Imidazolidin-2-yl)imino]-1H-indoles as new hypotensive agents: synthesis and in vitro and in vivo biological studies
Kornicka, Anita,Wasilewska, Aleksandra,S?czewski, Jaros?aw,Hudson, Alan L.,Boblewski, Konrad,Lehmann, Artur,Gzella, Karol,Belka, Mariusz,S?czewski, Franciszek,Gdaniec, Maria,Rybczyńska, Apolonia,B?czek, Tomasz
, p. 400 - 410 (2017/04/03)
A series of 1-[(imidazolidin-2-yl)imino]-1H-indole analogues of hypotensive α2-AR agonists, 1-[(imidazolidin-2-yl)imino]-1H-indazoles, was synthesized and tested in vitro for their activities at α1- and α2-adrenoceptors as well as imidazoline I1 and I2 receptors. The most active 1-[(imidazolidin-2-yl)imino]-1H-indoles displayed high or moderate affinities for α1- and α2-adrenoceptors and substantial selectivity for α2-adrenoceptors over imidazoline-I1 binding sites. The in vivo cardiovascular properties of indole derivatives 3 revealed that substitution at C-7 position of the indole ring may result in compounds with high cardiovascular activity. Among them, 7-fluoro congener 3g showed the most pronounced hypotensive and bradycardic activities in this experiment at a dose as low as 10?μg/kg i.v. Metabolic stability of the selected compounds of type 3 was determined using both in vitro and in silico approaches. The results indicated that these compounds are not vulnerable to rapid first-phase oxidative metabolism.
PYRIMIDINE HYDRAZIDE COMPOUNDS AS PGDS INHIBITORS
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Page/Page column 123-124, (2008/12/04)
This invention is directed to a compound wherein R1, R2, R3, R4 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or