Rovnyak, George C. published the artcileDihydropyrimidine calcium channel blockers. 4. Basic 3-substituted-4-aryl-1,4-dihydropyrimidine-5-carboxylic acid esters. Potent antihypertensive agents, Product Details of C10H15NO, the publication is Journal of Medicinal Chemistry (1992), 35(17), 3254-63, database is CAplus and MEDLINE.
A series of novel dihydropyrimidine calcium channel blockers that contain a basic group attached to either C(5) or N(3) of the heterocyclic ring has been examined Structure-activity studies show that a 1-(phenylmethyl)-4-piperidinyl carbamate moiety at N(3) and sulfur at C(2) are optimal for vasorelaxant activity in vitro and impart potent and long-acting antihypertensive activity in vivo. One of the title compounds was identified as a lead, and the individual enantiomers (R)- and (S)-I were synthesized. Two key steps of the synthesis were the efficient separation of their diastereomeric ureido derivatives and the high-yield transformation of 2-methoxy intermediates into 2-(p-methoxybenzyl)thio intermediates. Chirality was demonstrated to be a significant determinant of biol. activity, with the dihydropyridine receptor recognizing the enamino ester moiety (R)-I but not the carbamate moiety (S)-I. Dihydropyrimidine (R)-I is equipotent to nifedipine and amlodipine in vitro. In the spontaneously hypertensive rat, (R)-I is both more potent and longer acting than nifedipine and compares most favorably with the long-acting dihydropyridine derivative amlodipine. (R)-I has the potential advantage of being a single enantiomer.
Journal of Medicinal Chemistry published new progress about 101-98-4. 101-98-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Alcohol, name is 2-(Benzyl(methyl)amino)ethanol, and the molecular formula is C10H15NO, Product Details of C10H15NO.
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