By Annette M. Doherty
Annual stories in Medicinal Chemistry maintains to target offering well timed and significant reports of vital issues in medicinal chemistry including an emphasis on rising issues within the organic sciences, that are anticipated to supply the root for solely new destiny remedies. Sections I-IV are ailment oriented and customarily document on particular medicinal brokers. Sections V and VI proceed to stress very important themes in medicinal chemistry, biology, and drug layout. * Annual accomplished studies of the earlier yr literature in lots of subject matters of curiosity to medicinal chemists * contains a accomplished set of indices to simply find issues in Volumes 1-38 of this sequence * offers serious evaluation on sizzling subject matters in medicinal chemistry
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Extra resources for Annual Reports in Medicinal Chemistry, Vol. 39
Interestingly, Novartis researchers did not observe lowered glucose levels with their PDHK inhibitors, for example 21, in rodent models of type 2 diabetes [16,17], but observed significantly diminished blood lactate levels. 2. Liver-selective glucocorticoid receptor antagonist The correlation between elevated hepatic glucose output and fasting hyperglycemia in type 2 diabetic patients is well established. Also, the link between elevated glucocorticoids (GCs) and their role in glucose control suggested the desirability of exploring glucocorticoid receptor antagonism as a potential therapy for T2D.
The potent RXR modulator LG100268, 10, activates the RXR:PPAR-g heterodimer as efficiently as the PPAR-g agonist (BRL-49653 – rosiglitazone) in in vitro assays. Compound 10, was found to improve glucose tolerance in Zucker female fa/fa rats and also restrained weight gain in a 6 week study relative to the PPAR-g agonist BRL-49653. However, 10 was found to raise triglyceride levels 2 h post-dose, and to lower TSH levels 24 h postdose in Sprague Dawley rats following a single administration of 10 or 30 mg/kg, po.
L. Faulkner, T. A. Grese, R. A. Heyman, D. S. Karanewsky, K. Klausing, M. D. Leibowitz, S. Liu, D. A. Mais, C. M. Mapes, K. B. Marschke, A. Reifel-Miller, K. M. Ogilvie, D. Rungta, A. W. Thompson, J. S. Tyhonas and M. F. Boehm, J. Med. , 2003, 46, 2683.  P. Y. Michellys, M. F. Boehm, J. H. Chen, T. A. Grese, D. S. Karanewsky, M. D. Leibowitz, S. Liu, D. A. Mais, C. M. Mapes, A. Reifel-Miller, K. M. Ogilvie, D. Rungta, A. W. Thompson, J. S. Tyhonas, N. Yumibe and R. J. Ardecky, Bioorg. Med. Chem.
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