161493-22-7Relevant articles and documents
Enantioselective organocatalytic partial transfer hydrogenation of lactone-fused quinolines
Aillerie, Alexandre,Talance, Vincent Lemau De,Moncomble, Aurelien,Bousquet, Till,Pelinski, Lydie
supporting information, p. 2982 - 2985 (2014/06/23)
The first enantioselective synthesis of 4-aza-podophyllotoxin derivatives by partial transfer hydrogenation of lactone-fused quinolines was achieved using a chiral Bronsted acid catalyst. This reaction was extended to a large scope of substrates with good yields and enantioselectivities.
Studies on disease-modifying antirheumatic drugs. III. Bone resorption inhibitory effects of ethyl 4-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4- triazol-1-ylmethyl)quinoline-3-carboxylate (TAK-603) and related compounds
Baba, Atsuo,Oda, Tsuneo,Taketomi, Shigehisa,Notoya, Kohei,Nishimura, Atsushi,Makino, Haruhiko,Sohda, Takashi
, p. 369 - 374 (2007/10/03)
In the course of our studies aimed at obtaining new drugs for treatment of bone and joint diseases, chemical modification of the potent bone resorption inhibitors justicidins, was performed and various naphthalene lactones, quinoline lactones and quinoline derivatives bearing an azole moiety at the side chain were prepared. Their inhibitory effects on bone resorption were evaluated by Raisz's method, and several compounds, including ethyl 4-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1- ylmethyl)quinoline-3-arboxylate (6c, TAK-603), were found to have activities comparable with or superior to the justicidins. The 4-(3-isopropoxy-4- methoxy)phenyl derivative (6d), in particular, displayed a marked increase in potency. TAK-603 and compound 6d were very effective in preventing osteoclast formation and bone resorption by mature osteoelasts. Further, TAK-603 was shown to be effective in preventing bone loss in ovariectomized mice.
