683273-33-8Relevant academic research and scientific papers
A New Series of Highly Potent Non-Peptide Bradykinin B2 Receptor Antagonists Incorporating the 4-Heteroarylquinoline Framework. Improvement of Aqueous Solubility and New Insights into Species Difference
Sawada, Yuki,Kayakiri, Hiroshi,Abe, Yoshito,Imai, Keisuke,Mizutani, Tsuyoshi,Inamura, Noriaki,Asano, Masayuki,Aramori, Ichiro,Hatori, Chie,Katayama, Akira,Oku, Teruo,Tanaka, Hirokazu
, p. 1617 - 1630 (2007/10/03)
Introduction of nitrogen-containing heteroaromatic groups at the 4-position of the quinoline moiety of our non-peptide B2 receptor antagonists resulted in enhancing binding affinities for the human B 2 receptor and reducing binding affinities for the guinea pig one, providing new structural insights into species difference. A CoMFA study focused on the diversity of the quinoline moiety afforded correlative and predictive QSAR models of binding for the human B2 receptor but not for the guinea pig one. A series of 4-(1-imidazolyl)quinoline derivatives could be dissolved in a 5% aqueous solution of citric acid up to a concentration of 10 mg/mL. A representative compound 48a inhibited the specific binding of [ 3H]BK to the cloned human B2 receptor expressed in Chinese hamster ovary cells with an IC50 value of 0.26 nM and significantly inhibited BK-induced bronchoconstriction in guinea pigs even at 1 μg/kg by intravenous administration.
Quinoline derivatives, processes for their preparation and their use as medicaments
-
, (2008/06/13)
PCT No. PCT/JP97/01415 Sec. 371 Date Oct. 26, 1998 Sec. 102(e) Date Oct. 26, 1998 PCT Filed Apr. 24, 1997 PCT Pub. No. WO97/15877 PCT Pub. Date Apr. 24, 1997A compound of the formula: wherein R1 is lower alkyl, R2 is hydrogen, lower alkyl or a heterocyclic group, R3 is hydrogen, lower alkyl or halogen, R4 is lower alkyl or halogen, R5 is nitro or amino substituted with substituent(s) selected from the group consisting of lower alkyl and acyl, and A is lower alkylene.
