90445-15-1Relevant articles and documents
Long-acting dihydropyridine calcium antagonists. 3. Synthesis and structure-activity relationships for a series of 2-[(heterocyclylmethoxy) methyl]derivatives
Alker,Campbell,Cross,Burges,Carter,Gardiner
, p. 2381 - 2388 (1989)
The preparation of 1,4-dihydropyridines containing (heterocyclylmethoxy)methyl groups in the 2-position is described and the structural identification of certain of the compounds using 1H NMR spectroscopic methods is reported. The calcium antagonist activity of the compounds on rat aorta is listed and is compared with the negative inotropic potency as determined by using a Langendorff-perfused guinea pig heart model. Several compounds are more potent than nifedipine and show greater selectivity for the vasculature over the heart. One compound, 2-[[(2-amino-4-hydroxypyrimidin-6-yl)methoxy]methyl]-4-(2,3- dichlorophenyl)-3-(ethoxycarbonyl)-5-(methoxycarbonyl)-6-methyl-1,4- dihydropyridine (27, UK-56,593), was identified as a potent (IC50 = 1.6 x 10-9 M), tissue-selective calcium antagonist which proved to have a markedly longer duration of action (>4.5 h) than nifedipine in the anesthetized dog on intravenous administration.
Dihydropyridine anti-ischaemic and antihypertensive agents
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, (2008/06/13)
1,4-Dihydropyridine derivatives of the formula: STR1 wherein R is aryl or heteroaryl: R1 and R2 are each independently C1 -C4 alkyl or 2-methoxyethyl; Y is --(CH2)n --, --CH2 CH(CH3)-- or --CH2 C(CH3)2 --; n is 1 to 3; and X is a 5 or 6 membered nitrogen containing aromatic heterocyclic ring which may optionally be substituted by one or more C1 -C4 alkyl, phenyl, benzyl, CN, --N(R3)2, (CH2)m CO2 H, (CH2)m CO2 (C1 -C4 alkyl) or (CH2)m CON(R3)2 group wherein each R3 is independently H or C1 -C4 alkyl and m is 0 or 1; and their pharmaceutically acceptable acid addition salts, and pharmaceutical preparation containing such compounds, have utility as anti-ischaemic and antihypertensive agents.
Dihydropyridine anti-ischaemic and antihypertensive agents
-
, (2008/06/13)
1,4-Dihydropyridine derivatives of the formula: STR1 wherein R is aryl or heteroaryl; R1 and R2 are each independently C1 -C4 alkyl or 2-methoxyethyl; Y is --(CH2)n --, --CH2 CH(CH3)-- or --CH2 C(CH3)2 13 ; n is 1 to 3; and X is a 5 or 6 membered nitrogen containing aromatic heterocyclic ring which may optionally be substituted by one or more C1 -C4 alkyl, phenyl, benzyl, CN, --N(R3)2, (CH2)m CO2 H, (CH2)m CO2 (C1 -C4 alkyl) or (CH2)m CON(R3)2 group wherein each R3 is independently H or C1 -C4 alkyl and m is 0 or 1; and their pharmaceutically acceptable acid addition salts, and pharmaceutical preparation containing such compounds, have utility as anti-ischaemic and antihypertensive agents.
