14901-11-2Relevant academic research and scientific papers
OPIOID RECEPTOR MODULATORS AND USE THEREOF
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Paragraph 0050; 0222; 0223; 0389; 0390; 0391, (2017/03/21)
Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method
Design, synthesis and evaluation of 2-aminothiazole derivatives as sphingosine kinase inhibitors
Vogt, Dominik,Weber, Julia,Ihlefeld, Katja,Brüggerhoff, Astrid,Proschak, Ewgenij,Stark, Holger
, p. 5354 - 5367 (2014/12/11)
Sphingosine kinases (SphK1, SphK2) are main regulators of sphingosine-1-phosphate (S1P), which is a pleiotropic lipid mediator involved in numerous physiological and pathophysiological functions. SphKs are targets for novel anti-cancer and anti-inflammatory agents that can promote cell apoptosis and modulate autoimmune diseases. Herein, we describe the design, synthesis and evaluation of an aminothiazole class of SphK inhibitors. Potent inhibitors have been discovered through a series of modifications using the known SKI-II scaffold to define structure-activity relationships. We identified N-(4-methylthiazol-2-yl)-(2,4′-bithiazol)-2′-amine (24, ST-1803; IC50values: 7.3 μM (SphK1), 6.5 μM (SphK2)) as a promising candidate for further in vivo investigations and structural development.
Pyrimidinone antibiotics - Heterocyclic analogues with improved antibacterial spectrum
Brands, Michael,Grande, Yolanda Cancho,Endermann, Rainer,Gahlmann, Reinhold,Krueger, Jochen,Raddatz, Siegfried
, p. 2641 - 2645 (2007/10/03)
We report the synthesis and pharmacological evaluation of new derivatives of the natural dipeptide antibiotic TAN 1057 A,B containing heterocycles either in the β-amino acid side chain or as mimics of the urea function. In the course of this program, we identified novel analogues that display activity towards a broader panel of Gram-positive bacteriae.
