253595-70-9Relevant articles and documents
Tryptophan-containing dipeptide derivatives as potent PPARγ antagonists: Design, synthesis, biological evaluation, and molecular modeling
Deng, Guanghui,Liu, Zhiguo,Ye, Fei,Luo, Xiaomin,Zhu, Weiliang,Shen, Xu,Liu, Hong,Jiang, Hualiang
experimental part, p. 2699 - 2716 (2009/04/11)
The discovery of peroxisome proliferator-activated receptor γ (PPARγ) antagonists (also termed "selective PPARγ modulators, SPPARγM") is now of a great interest in the treatment of diabetes and obesity. The structure of compound 1a (G3335, Fig. 1), a novel class of PPARγ antagonist, is entirely different from that of other reported PPARγ antagonists. A series of 35 novel analogues (1b-l, 9a-d, 13a-t) were designed, synthesized and evaluated against the agonistic effects exerted by rosiglitazone. These results indicated that most functional groups of 1a were conserved, and six new compounds (1b, 1c, and 9a-d) exhibited strong PPARγ antagonistic activities (IC50 values of 5.2-25.8 μM) against 10 μM rosiglitazone in the promotion of the PPARγ-LBD-CBP (ligand-binding domain and cAMP-response-element binding protein) interaction as investigated by yeast two-hybrid technology based assay. Molecular modeling studies for compounds 1a-d, 1h, 9c-d, and 13a were also presented.
Tetrahydropyran-amino acids: Novel building blocks for gramicidin-hybrid ion channels
Schr?der, Sabine,Schrey, Anna K.,Knoll, Andrea,Rei?, Philipp,Ziemer, Burkhard,Koert, Ulrich
, p. 2766 - 2776 (2007/10/03)
The stereoselective synthesis of a cis-2,6-disubstituted tetrahydropyran bearing a δ-amino acid has been achieved starting from N-Boc-leucinal. The THP amino acid was incorporated into peptide sequences and the structural consequences were studied by X-ra
Synthesis and functional studies of THF-gramicidin hybrid ion channels
Vescovi, Andrea,Knoll, Andrea,Koert, Ulrich
, p. 2983 - 2997 (2007/10/03)
THF-gramicidin hybrids 2-4 with the L-THF amino acid 1 in positions 11 and 12 and compounds 5-8 with the D-THF amino acid ent-1 in positions 10 and 11 were synthesized and their ion channel properties were studied by single-channel-current analysis. The r
Solution phase synthesis and purification of the minigramicidin ion channels and a succinyl-linked gramicidin
Arndt, Hans-Dieter,Vescovi, Andrea,Schrey, Anna,Pfeifer, Jochen R,Koert, Ulrich
, p. 2789 - 2801 (2007/10/03)
Peptides with alternating D- and L-configured residues as found in the natural ion channel active peptide gramicidin A (gA) are important building blocks for artificially engineered ion channels. We detail an optimised solution phase synthesis employing a