- Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels
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Cilnidipine is a 1,4-dihydropyridine derived L/N-type calcium channel dual blocker possessing neuroprotective and analgesic effects which are related to its N-type calcium channel inhibitory activity. In order to find specific N-type calcium channel blockers with the least effects on cardiovascular system, we performed structure-activity relationship study on APJ2708, which is a derivative of cilnidipine, and found a promising N-type calcium channel blocker 21b possessing analgesic effect in vivo with a 1600-fold lower activity against L-type calcium channels than that of cilnidipine.
- Yamamoto, Takashi,Niwa, Seiji,Ohno, Seiji,Onishi, Tomoyuki,Matsueda, Hiroyuki,Koganei, Hajime,Uneyama, Hisayuki,Fujita, Shin-Ichi,Takeda, Tomoko,Kito, Morikazu,Ono, Yukitsugu,Saitou, Yuki,Takahara, Akira,Iwata, Seinosuke,Shoji, Masataka
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p. 798 - 802
(2007/10/03)
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- Process for preparing 1,4 dihydropyridine compounds
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A 1,4-dihydropyridine derivative represented by formula (I): STR1 wherein X represents an alkyl group, or a group of STR2 in which R1, R2, and R3 may be the same or different and each represent a hydrogen atom, a halogen atom, a nitro group, a nitrile group, or a trifluoromethyl group; R4 represents a substituted or unsubstituted acyloxymethyl group, an alkoxycarbonyloxymethyl group, a (2-oxo-1,3-dioxolen-4 -yl)methyl group, a (5-substituted-2-oxo-1,3-dioxolen-4 -yl)methyl group, or an acyl group; R5 represents a lower alkyl group or a substituted alkyl group; and R6 represents a hydrogen atom, a lower alkoxymethyl group, or a lower acyloxymethyl group, is disclosed. The compound is stereospecifically hydrolyzed by the action of an enzyme to provide an optically active 1,4-dihydro -3-pyridinemonocarboxylic acid which is useful as an intermediate of pharmaceuticals in good optical purity and yield.
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- Isomers of 1-azabicyclo(2.2.2)oct-3-yl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-5-nitropyridine-3-carboxylate
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The four stereoisomers are disclosed having the formula: STR1 in which the asymmetric centers a and b are the same or different. The compounds are derived from the (+) and (-) alcohols and the (+) and (-) dihydropyridines and have either the absolute R or
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