Laeckmann, Didier; Rogister, Francoise; Dejardin, Jean-Victor; Prosperi-Meys, Christelle; Geczy, Joseph; Delarge, Jacques; Masereel, Bernard published the artcile< Synthesis and biological evaluation of aroylguanidines related to amiloride as inhibitors of the human platelet Na+/H+ exchanger>, Product Details of C6H2Cl3NO2, the main research area is pyridine benzene isostere amiloride preparation sodium hydrogen exchanger inhibitor; structure amiloride isostere activity inhibitor sodium hydrogen exchanger.
Pyridine and benzene bioisosteres of amiloride such as I and II were synthesized and evaluated for their inhibitory potency against the sodium-hydrogen exchanger involved in intracellular pH regulation. Substituted diaminochloro-2-pyridinecarbonyl and diaminochloro-3-pyridinecarbonyl guanidines are prepared from 2-chloro-6-methyl-3,5-dinitropyridine and 2-methyl-1,5-pentanedinitrile, resp. Dichloro- and trichloropyridine-3-carbonyl guanidines, and simple pyridinecarbonyl and benzoyl guanidines are also prepared Several benzene derivatives and compounds bearing an carbonylguanidine moiety in the meta position of the pyridine nitrogen were much more potent than amiloride, but less so than the pyrazine inhibitor III (R = Et; R1 = Me2CH). II is the most active mol. in assays measuring the reduction in human platelet swelling due to sodium ion uptake and in assays of the inhibition of sodium ion uptake, with IC50 values of 0.8 μM in both assays. Replacement of the pyrazine ring of amiloride III (R = R1 = H) by a pyridine or a Ph ring improved the inhibitory potency for the sodium-hydrogen exchanger involved in intracellular pH regulation in the order Ph > pyridine > pyrazine.
Bioorganic & Medicinal Chemistry published new progress about Homo sapiens. 54718-39-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H2Cl3NO2, Product Details of C6H2Cl3NO2.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics