247569-76-2Relevant academic research and scientific papers
Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors
Koltun, Dmitry O.,Vasilevich, Natalya I.,Parkhill, Eric Q.,Glushkov, Andrei I.,Zilbershtein, Timur M.,Mayboroda, Elena I.,Boze, Melanie A.,Cole, Andrew G.,Henderson, Ian,Zautke, Nathan A.,Brunn, Sandra A.,Chu, Nancy,Hao, Jia,Mollova, Nevena,Leung, Kwan,Chisholm, Jeffrey W.,Zablocki, Jeff
scheme or table, p. 3050 - 3053 (2010/01/16)
We discovered a structurally novel SCD (Δ9 desaturase) inhibitor 4a (CVT-11,563) that has 119 nM potency in a human cell-based (HEPG2) SCD assay and selectivity against Δ5 and Δ6 desaturases. This compound has 90% oral bioavailability (rat) and excellent
Anthranilic acid derivatives as inhibitors of the cGMP-phosphodiesterase
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, (2008/06/13)
Compounds of formula (I) STR1where R 1 is hydrogen; R 2 is nitro, cyano or halo(lower)alkyl; R 3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R 4 is a group CR 6 R 7 R 8 wherein R 6 and R 7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R 8 is hydrogen; its prodrug and a salt thereof.
