852145-99-4Relevant academic research and scientific papers
Shedding X-ray Light on the Role of Magnesium in the Activity of Mycobacterium tuberculosis Salicylate Synthase (MbtI) for Drug Design
Mori, Matteo,Stelitano, Giovanni,Gelain, Arianna,Pini, Elena,Chiarelli, Laurent R.,Sammartino, José C.,Poli, Giulio,Tuccinardi, Tiziano,Beretta, Giangiacomo,Porta, Alessio,Bellinzoni, Marco,Villa, Stefania,Meneghetti, Fiorella
, p. 7066 - 7080 (2020/07/28)
The Mg2+-dependent Mycobacterium tuberculosis salicylate synthase (MbtI) is a key enzyme involved in the biosynthesis of siderophores. Because iron is essential for the survival and pathogenicity of the microorganism, this protein constitutes an attractiv
Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation
Pismataro, Maria Chiara,Horenstein, Nicole A.,Stokes, Clare,Quadri, Marta,De Amici, Marco,Papke, Roger L.,Dallanoce, Clelia
, (2020/08/19)
The α7 nicotinic acetylcholine receptor (nAChR) silent agonists, able to induce receptor desensitization and promote the α7 metabotropic function, are emerging as new promising therapeutic anti-inflammatory agents. Herein, we report the structure–activity
PHENYLALANINE DERIVATIVES AND THEIR USE AS NON-PEPTIDE GLP-1 RECEPTOR MODULATORS
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Page/Page column 34, (2012/01/14)
Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metab
Discovery of new C3aR ligands. Part 1: Arginine derivatives
Denonne, Frederic,Binet, Sophie,Burton, Maggi,Collart, Philippe,Dipesa, Alan,Ganguly, Tanmoy,Giannaras, Alexander,Kumar, Seema,Lewis, Timothy,Maounis, Florence,Nicolas, Jean-Marie,Mansley, Tamsin,Pasau, Patrick,Preda, Dorin,Stebbins, Karin,Volosov, Alexander,Zou, Dong
, p. 3258 - 3261 (2008/02/08)
The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflamma
FURANCARBONYLGUANIDINE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page/Page column 13, (2010/02/12)
The present invention relates to furancarbonylguanidine derivatives, a preparation method thereof and a pharmaceutical composition comprising the same. Furancarbonylguanidine derivatives of the present invention inhibit NHE-1 (sodium-hydrogen exchanger isoform 1), which helps recovery of heart function damaged from ischemia/ reperfusion and decreases myocardial infarction rate, indicating that they have protective effect on myocardial cells. Thus, furancarbonylguanidine derivatives of the present invention can be ef-fectively used for the prevention and the treatment of ischemic heart diseases such as myocardial infarction, arrhythmia, angina pectoris, etc, and also a promising candidate for a heart protecting agent applied to reperfusion therapy including thrombolytics or cardiac surgery including coronary artery bypass graft, percutaneous transluminal coronary angioplasty, etc.
(5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1
Lee, Sunkyung,Yi, Kyu Yang,Hwang, Sun Kyung,Lee, Byung Ho,Yoo, Sung-Eun,Lee, Kyunghee
, p. 2882 - 2891 (2007/10/03)
A series of (5-arylfuran-2-ylcarbonyl)guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardiprotective efficacy against ischemia-reperfusion injury. Starting with (5-phenylfuran-2-ylcarbonyl) guanidine 47 with a moderate inhibitory effect on NHE-1, the compounds with various substituents at the phenyl ring were investigated with the aim to optimize the potency. In this study, the 2,5-disubstituted compounds appeared to have better activities than the other analogues, and the 2-methoxy-5- chlorophenyl compound 85 was found as a potent inhibitor of NHE-1 (IC 50 = 0.081 μM). Furthermore, 85 showed a marked reduction of infarct size in the rat myocardial infarction model in vivo and significant improvement of cardiac contractile function in the isolated rat heart ischemia model in vitro.
