Safety of Ethyl 2-amino-2-thioxoacetateIn 2010 ,《Novel Bisaryl Substituted Thiazoles and Oxazoles as Highly Potent and Selective Peroxisome Proliferator-Activated Receptor δ Agonists》 was published in Journal of Medicinal Chemistry. The article was written by Epple, Robert; Cow, Christopher; Xie, Yongping; Azimioara, Mihai; Russo, Ross; Wang, Xing; Wityak, John; Karanewsky, Donald S.; Tuntland, Tove; Nguyen-Tran, Van T. B.; Cuc Ngo, Cara; Huang, David; Saez, Enrique; Spalding, Tracy; Gerken, Andrea; Iskandar, Maya; Seidel, H. Martin; Tian, Shin-Shay. The article contains the following contents:
The discovery, synthesis, and optimization of compound I from a high-throughput screening hit to highly potent and selective peroxisome proliferator-activated receptor δ (PPARδ) agonists are reported. The synthesis and structure-activity relationship in this series are described in detail. On the basis of a general schematic PPAR pharmacophore model, scaffold I was divided into headgroup, linker, and tailgroup and successively optimized for PPAR activation using in vitro PPAR transactivation assays. A (2-methylphenoxy)acetic acid headgroup, a flexible linker, and a five-membered heteroaromatic center ring with two hydrophobic aryl substituents were required for efficient and selective PPARδ activation. The fine-tuning of these aryl substituents led to an array of highly potent and selective compounds such as compound II, displaying an excellent pharmacokinetic profile in mouse. In an in vivo acute dosing model, selected members of this array were shown to induce the expression of pyruvate dehydrogenase kinase-4 (PDK4) and uncoupling protein-3 (UCP3), genes that are known to be involved in energy homeostasis and regulated by PPARδ in skeletal muscle. In addition to this study using Ethyl 2-amino-2-thioxoacetate, there are many other studies that have used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Safety of Ethyl 2-amino-2-thioxoacetate) was used in this study.
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Safety of Ethyl 2-amino-2-thioxoacetate
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