Ostacolo, Carmine published the artcileSynthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators, Application of ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, the publication is Journal of Medicinal Chemistry (2020), 63(1), 163-185, database is CAplus and MEDLINE.
Kv7 K+ channels represent attractive pharmacol. targets for the treatment of different neurol. disorders, including epilepsy. In this paper, 42 conformationally restricted analogs of the prototypical Kv7 activator retigabine have been synthesized and tested by electrophysiol. patch-clamp experiments as Kv7 agonists. When compared to retigabine (0.93 ± 0.43 μM), the EC50s for Kv7.2 current enhancements by compound I (0.08 ± 0.04 μM) were lower, whereas no change in potency was observed for II (0.63 ± 0.07 μM). In addition, compared to retigabine, I and II showed also higher potency in activating heteromeric Kv7.2/Kv7.3 and homomeric Kv7.4 channels. Mol. modeling studies provided new insights into the chem. features required for optimal interaction at the binding site. Stability studies evidenced improved chem. stability of I and II in comparison with retigabine. Overall, the present results highlight that the N5-alkylamidoindole moiety provides a suitable pharmacophoric scaffold for the design of chem. stable, highly potent and selective Kv7 agonists.
Journal of Medicinal Chemistry published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C10H15ClO3S, Application of ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride.
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