Luo, Zonghua published the artcileDesign and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands, Application of 2-Chloro-6-methoxyisonicotinoyl chloride, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(3), 488-496, database is CAplus and MEDLINE.
Eleven new sphingosine 1-phosphate receptor 2 (S1PR2) ligands were synthesized by modifying lead compound N-(2,6-dichloropyridin-4-yl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazine-1-carboxamide (I, JTE-013) and their binding affinities toward S1PRs were determined in vitro using [32P]S1P and cell membranes expressing recombinant human S1PRs. Among these ligands, 35a (II, IC50 = 29.1 ± 2.6 nM) and 35b (III, IC50 = 56.5 ± 4.0 nM) exhibit binding potency toward S1PR2 comparable to JTE-013 (IC50 = 58.4 ±7.4 nM) with good selectivity for S1PR2 over the other S1PRs (IC50 > 1000 nM). Further optimization of these analogs may identify addnl. and more potent and selective compounds targeting S1PR2.
Bioorganic & Medicinal Chemistry Letters published new progress about 116853-97-5. 116853-97-5 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,acyl chloride,Ether, name is 2-Chloro-6-methoxyisonicotinoyl chloride, and the molecular formula is C7H5Cl2NO2, Application of 2-Chloro-6-methoxyisonicotinoyl chloride.
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