173776-64-2Relevant academic research and scientific papers
Diarylspiro[2.4]heptenes as orally active, highly selective cyclooxygenase-2 inhibitors: Synthesis and structure-activity relationships
Huang, Horng-Chih,Li, James J.,Garland, Danny J.,Chamberlain, Timothy S.,Reinhard, Emily J.,Manning, Robert E.,Seibert, Karen,Koboldt, Carol M.,Gregory, Susan A.,Anderson, Gary D.,Veenhuizen, Amy W.,Zhang, Yan,Perkins, William E.,Burton, Earl G.,Cogburn, J. Nita,Isakson, Peter C.,Reitz, David B.
, p. 253 - 266 (1996)
A novel series of 5,6-diarylspiro[2.4]hept-5-enes was shown to provide highly potent and selective cyclooxygenase-2 (COX-2) inhibitors. A study of structure-activity relationships in this series suggests that 3,4- disubstituted phenyl analogs are generally more selective than 4-substituted phenyl analogs and that replacement of the methyl sulfone group on the 6- phenyl ring with a sulfonamide moiety results in compounds with superior in vivo pharmacological properties, although with lower COX-2 selectivity. Several compounds have been shown to possess promising pharmacological properties in adjuvant-induced arthritis and edema analgesia models. The absence of gastrointestinal (GI) toxicity at 200 mpk of several selected compounds in rats and mice corresponds well with the weak potency for inhibition of COX-1 observed in the enzyme assay. Methyl sulfone 55 and sulfonamide 24 were shown to have superior in vivo pharmacological profiles, low GI toxicity, and good oral bioavailability and duration of action.
Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors
Lee, Ki-Ho,Park, Chun-Eung,Min, Kyung-Hyun,Shin, Yong-Je,Chung, Coo-Min,Kim, Hui-Ho,Yoon, Hae-Jeoung,Won-Kim,Ryu, Eun-Ju,Shin, Yu-Jin,Nam, Hyun-Sik,Cho, Jeong-Woo,Lee, Hee-Yoon
scheme or table, p. 5567 - 5571 (2010/12/29)
A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In
