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Thyroid hormone analogues

Structure—Activity Relationships. In spite of the considerable synthetic and bioassay effort involved in estabhshing the thyromimetic potency of thyroid-hormone analogues, more than 100 compounds have been studied (Table 2). The main stmctural requirements for thyromimetic activity can be summarized as follows (6,12—16). [Pg.48]

A large number of thyroid hormone analogues have been tested for this effect (6). Among others, i-T (3) and 3,3 -T2 (5) and their propionic acid side-chain analogues decrease oxygen consumption at molar ratios of 50—200 1 of T. Nevertheless, no potent or clinically usehil peripheral antagonists have been found. [Pg.53]

Within a programme aimed at the development of thyroid hormone analogues as potentially useful plasma cholesterol-lowering agents, the pyrida-zinone derivative SK F L-94901 (98) has been prepared and investigated in the U.K. [419-422]. Whereas naturally occurring thyroid hormones cannot be employed for this purpose because of their undesirable effect on heart rate, (98) has been found to represent a potent thyromimetic which retains hepatic activity but lacks cardiac activity. Structural modifications and QSAR studies have been carried out [422]. [Pg.163]

Chiellini, G. Nguyen, N.-H. Apriletti, J. W. Baxter, J. D. Scanlan, T. S. Synthesis and biological activity of novel thyroid hormone analogues 5 -aryl substituted GC-1 derivatives. Bioorg. Med. Chem. 2002, 10, 333—346. [Pg.256]

Mousa SA, O Connor LJ, Bergh JJ, et al, The proangiogenic action of thyroid hormone analogue GC-I is initiated at an integrin, J Cardiovasc Pharmacol 2005 46 356-360,... [Pg.403]

K. W. Mahaffey, T.E. Raya, G.D. Pennock, E. Morkin and S. Goldman, Left ventricular performance and remodeling in rabbits after myocardial infarction effects of a thyroid hormone analogue, Circulation 91(3), 794-801 (1995). [Pg.97]

We next apphed the method of MaNP acid 3, which is very effective for enantior-esolving racemic alcohols and also for determining the absolute configuration of chiral alcohols by the H NMR anisotropy method as described above. We explain here the apphcation of the MaNP acid method to the chiral thyroid hormone analogue KAT-2003 (-i-)-9 to determine its absolute configuration. [Pg.316]

Leeson, P.D., Ellis, D., Emmett, J.C., Shah, V.P., Showell. G.A., and Underwood, A.H., Thyroid hormone analogues. Synthesis of 3 -substituted 3,5-diiodo-L-thyronines and quantitative structure-activity studies of in vivo thyromimetic activities in rat liver and heart, J. Med. Chem., 31, 37, 1988. [Pg.312]

The search for thyroid hormone analogues was prompted by the desire to establish SARs for the hormone and by the need for a safe, specific antagonist able to block thyroid action without delay at a peripheral site. The reader will recall that TPO inhibitors, such as PTU, do not affect the extensive amount of hormone stored in thyroidal thyroglobulin. [Pg.1382]

Leeson PD, Ellis D, Emmett JC, et al. Thyroid hormone analogues. Synthesis of 3 -substituted... [Pg.1398]

Kollman PA, Murray WJ, Nuss ME, et al. Molecular orbital studies of thyroid hormone analogues. J Am Chem Soc 1973 95 8518-8525. [Pg.1399]

Eprotirome (KB2115) is a thyroid hormone analogue that has modestly higher affinity for the triiodothyronine receptor p isoform (and mediates the lipid-lowering actions of thyroid hormone) compared with its affinity for the triiodothyronine receptor a isoform in the heart. [Pg.679]

Burridge, and C. C. F. Blake,/. Am. Chem. Soc., 104, 6424 (1982). Molecular Mechanics Simulation of Protein-Ligand Interactions Binding of Thyroid Hormone Analogues to Prealbumin. [Pg.239]

Nishimura T, Taji H, Harada N. Absolute configuration of the thyroid hormone analogue KAT-2003 as determined by the H NMR anisotropy method with a novel chiral auxiliary, MaNP acid. C/ >a/fty 2004 16 13-21. [Pg.1661]


See other pages where Thyroid hormone analogues is mentioned: [Pg.50]    [Pg.524]    [Pg.278]    [Pg.65]    [Pg.66]    [Pg.67]    [Pg.50]    [Pg.1502]    [Pg.941]    [Pg.329]    [Pg.315]    [Pg.1382]    [Pg.1388]   
See also in sourсe #XX -- [ Pg.926 , Pg.927 , Pg.928 , Pg.929 ]




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