84891-45-2Relevant academic research and scientific papers
Novel Phosphinic Acid-Containing Thyromimetics
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Page/Page column 97, (2009/02/11)
The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.
Identification of ACE pharmacophore in the phosphonopeptide metabolite K-26
Ntai, Ioanna,Bachmann, Brian O.
, p. 3068 - 3071 (2008/12/23)
The naturally occurring phosphonotripeptide K-26 is a potent angiotensin converting enzyme (ACE) inhibitor containing an α-amino phosphonic acid analogue of tyrosine. Previous studies have demonstrated that canonical peptide analogues of K-26 are micromolar inhibitors of ACE. To ascertain the structure-activity relationships in this class of ACE inhibitory natural products, K-26 and eight analogues were chemically synthesized and evaluated. Phosphonyl substitution was found to be the critical determinant of activity, resulting in a 1500-fold increase in ACE inhibition versus carboxyl analogues. Secondarily, the absolute configuration of the terminal α-amino phosphonate and N-acetylation were found to significantly modulate ACE inhibitory activity.
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs
Boyer, Serge H.,Jiang, Hongjian,Jacintho, Jason D.,Reddy, Mali Venkat,Li, Haiqing,Li, Wenyu,Godwin, Jennifer L.,Schulz, William G.,Cable, Edward E.,Hou, Jinzhao,Wu, Rongrong,Fujitaki, James M.,Hecker, Scott J.,Erion, Mark D.
experimental part, p. 7075 - 7093 (2009/11/30)
Phosphonic acid (PA) thyroid hormone receptor (TR) agonists were synthesized to exploit the poor distribution of PA-based drugs to extrahepatic tissues and thereby to improve the therapeutic index. Nine PAs showed excellent TR binding affinities (TRβ
NOVEL PHOSPHORUS-CONTAINING THYROMIMETICS
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Page/Page column 223, (2008/06/13)
The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.
