30413-58-2Relevant academic research and scientific papers
ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: Identification, in vitro pharmacology, pharmacokinetic and biodistribution studies
Hintermann, Samuel,Vranesic, Ivo,Allgeier, Hans,Bruelisauer, Armin,Hoyer, Daniel,Lemaire, Michel,Moenius, Thomas,Urwyler, Stephan,Whitebread, Steven,Gasparini, Fabrizio,Auberson, Yves P.
, p. 903 - 914 (2007)
[11C]ABP688 (2) has recently been demonstrated to be a useful PET tracer for in vivo imaging of the metabotropic glutamate receptors type 5 (mGluR5) in rodents. We describe here the identification and preclinical profiling of ABP688 and its tri
Design, synthesis, and biological evaluation of novel 2′-methyl-2′-fluoro-6-methyl-7-alkynyl-7-deazapurine nucleoside analogs as anti-Zika virus agents
Yao, Guoqiang,Yu, Jianchen,Lin, Cai,Zhu, Yujia,Duan, Anna,Li, Mengfeng,Yuan, Jie,Zhang, Jiancun
supporting information, (2022/03/23)
Zika virus (ZIKV) is a mosquito-borne flavivirus and outbreaks of ZIKV have been reported in Africa, Americas and other parts of the world lately. The ZIKV epidemic has received extensive attention due to its ability to cause serious medical consequences and complications such as microcephaly and Guillain-Barre syndrome in recent years. Up to now, there are no specific treatments or vaccines available for ZIKV infection, which highlights the urgent need for developing new therapies. In this work, we designed and synthesized a series of novel 6-methyl-7-acetylenenyl-7-deazapurine nucleoside analogs as potential inhibitors of ZIKV replication. The biological activities against ZIKV replication were evaluated and the structure-activity relationship (SAR) was also studied. Among the compounds evaluated, nucleoside analog 38 (EC50 = 2.8 ± 0.8 μM, EC90 = 6.8 ± 2.3 μM) showed the most potent anti-ZIKV activity with low cytotoxicity (CC50 = 54.1 ± 6.9 μM) in an A549 based cellular model. The inhibitory activity of 38 was about 5 times more potent than the positive control NITD008. Notably, 38 showed similar inhibition potency against different ZIKV strains (ZG-01 and MR766) in a variety of host cell types including SNB19, A549, Huh7, Vero. In addition, 38 (Kd = 1.87 μM) has a stronger affinity to ZIKV RNA-dependent RNA polymerase (RdRp) protein than NITD008 (Kd = 3.43 μM) in the non-phosphorylation assay. These results indicated that compound 38 may serve as a promising candidate in future anti-ZIKV drug discovery.
SUBSTITUTED 1,5-NAPHTHYRIDINES OR QUINOLINES AS ALK5 INHIBITORS
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, (2021/05/29)
The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
Palladium (II) complexes chelated by 1-substituted-4-pyridyl-1H-1,2,3-triazole ligands as catalyst precursors for selective ethylene dimerization
Joseph, Mohammed Cassiem,Swarts, Andrew John,Mapolie, Selwyn Frank
, (2020/03/03)
A series of neutral as well as cationic palladium methyl complexes bearing 1-substituted-4-pyridyl-1H-1,2,3-triazole ligands were prepared and fully characterized by a range of analytical techniques. Conventional and 2D NMR spectroscopy as well as single-crystal X-ray diffraction analysis unambiguously determined the molecular structure of the complexes. The neutral complexes activated by methylaluminoxane were found to be effective catalysts in the ethylene dimerization reaction. The catalyst performance of the in-situ-generated active species was compared with the discrete cationic complexes of the same ligand scaffold. Activities and selectivities for the two systems were remarkably similar, pointing to similarities in the nature of the active species. Both catalytic systems showed a strong correlation of activity and selectivity with the nature of the ligand scaffold. Highest activities were attained when electron-withdrawing groups were incorporated into the triazole ring, while increasing steric bulk in the ortho-position on the pyridyl ring of the ligand led to the almost exclusive dimerization of ethylene with selectivities up to 94% observed toward 1-butene.
NEW COMPOUND
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Paragraph 0316; 0320, (2019/11/26)
PROBLEM TO BE SOLVED: To provide a new compound that does not have structural similarity to ceramide and has excellent CERT inhibitory activity. SOLUTION: The present invention provides a new compound of structural formula (I). A bond group -X- is cis-cyclopropyl-, R1, R2, R3, R4, and R5 independently represent a hydrogen atom, a halogen atom, a linear or branched C1-C8 alkyl group that may have a halogen atom, or OR6. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPOandINPIT
STROBILURIN TYPE COMPOUNDS FOR COMBATING PHYTOPATHOGENIC FUNGI
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, (2015/01/07)
The present invention relates to novel strobilurine type compounds I, processes for preparing these compounds, a use of compounds of the formula I and/or their agriculturally useful salts for controlling phytopathogenic fungi, to compositions comprising at least one such compound, to plant health applications, and to seeds coated with at least one such compound.
Efficient synthesis of 2-pyridylenynes and application in cobalt-catalysed benzannulation reactions
R?se, Philipp,Pünner, Florian,Hilt, Gerhard,Harms, Klaus
, p. 1101 - 1104 (2013/06/27)
The cobalt-catalysed benzannulation of 2-pyridine-substituted enynes gave 2,3-bis(2-pyridyl)styrenes in moderate yields. The reaction with dibromomethane as well as diiodomethane generated the corresponding planar-chiral bispyridinium salts in good yields
Bicyclic piperazines as metabotropic glutatmate receptor antagonists
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Page/Page column 49, (2008/06/13)
The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, Hy, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR5-mediated disorders.
Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)
Bach, Peter,Nilsson, Karolina,Svensson, Tor,Bauer, Udo,Hammerland, Lance G.,Peterson, Alecia,Wallberg, Andreas,Oesterlund, Krister,Karis, David,Boije, Maria,Wensbo, David
, p. 4788 - 4791 (2007/10/03)
Studies of structure-activity relationships for the linker in a new series of metabotropic glutamate receptor 5 antagonists are presented together with in vitro and in vivo pharmacokinetic data.
Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity
Alagille, David,Baldwin, Ronald M.,Roth, Bryan L.,Wroblewski, Jarda T.,Grajkowska, Ewa,Tamagnan, Gilles D.
, p. 197 - 209 (2007/10/03)
Noncompetitive antagonists of the human metabotropic glutamate receptor subtype 5 (mGluR5) have been implicated as potential therapeutics for the treatment of a variety of nervous system disorders, including pain, anxiety, and drug addiction. To discover novel noncompetitive antagonists to the mGluR5, we initiated an SAR study around the known lead compounds MPEP and M-MPEP. Our results pointed out the critical role of the para position of the two aromatic rings, which leads to inactive products and permitted the discovery of potent mGluR5 antagonists (e.g., 16, 25, 28, 34 IC50 = 13.5, 11.9, 21, 15 nM, respectively). Noncompetitive antagonists of the human metabotropic glutamate receptor subtype 5 (mGluR5) have been implicated as potential therapeutics for the treatment of a variety of nervous system disorders, including pain, anxiety, and drug addiction. To discover novel noncompetitive antagonists to the mGluR5, we initiated an SAR study around the known lead compounds MPEP and M-MPEP. Our results pointed out the critical role of the para position of the two aromatic rings, which leads to inactive products and permitted the discovery of potent mGluR5 antagonists (e.g., 16, 25, 28, 34 IC50 = 13.5, 11.9, 21, 15 nM, respectively).
