- Synthesis and evaluation of α,α′-disubstituted phenylacetate derivatives for T-type calcium channel blockers
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We have synthesized and evaluated α,α′-disubstituted phenylacetate derivatives that were designed as T-type calcium channel blockers. Among them, compound 10e (IC50 = 8.17 ± 0.48 nM) showed the most potent T-type calcium current blocking activity and higher potency than Mibefradil (IC50 = 1.34 ± 0.49 μM). The PK profile and subtype selectivity over L-type calcium channel were satisfied for further animal assay using disease model.
- Lee, Hyung Kook,Lee, Yun Suk,Roh, Eun Joo,Rhim, Hyewhon,Lee, Jae Yeol,Shin, Kye Jung
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scheme or table
p. 4424 - 4427
(2009/04/06)
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- Tetrahydronaphthalene derivatives as calcium antagonists
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Compounds of the formula STR1 wherein R is lower-alkyl, R1 is halogen, R2 is C1 -C12 -alkyl, R3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylamin
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