74002-98-5Relevant articles and documents
Pyridyl ester containing 1,4-dihydropyridine derivatives and salts thereof and pharmaceutical composition containing the same
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, (2008/06/13)
This invention relates to a novel 1,4-dihydropyridine derivative of the formula STR1 wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharmaceutical compositions containing the same.
Highly selective inhibitors of thromboxane synthetase. 1. Imidazole derivatives
Iizuka,Akahane,Momose,Nakazawa,Tanouchi,Kawamura,Ohyama,Kajiwara,Iguchi,Okada,Taniguchi,Miyamoto,Hayashi
, p. 1139 - 1148 (2007/10/02)
The structure-activity relationships of imidazole derivatives as inhibitors of thromboxane (TX) synthetase were investigated. Introduction of various substituents (e.g., one or two methyl groups, a halogen atom, a methylidene group, unsaturated bonds, or a phenylene group) into the α position or other positions in the carboxy-bearing side chain of 1-(7-carboxyheptyl)imidazole was found to increase the inhibitory potency. The length of the side chains with the phenylene group was optimum for the inhibitory potency on TX synthetase in the region of 8.5-9.0 A. Among the tested imidazole derivatives, 1-(7-carboxy-7-methyl-2-octynyl)imidazole, 4-[3-(1-imidazolyl)-propyl]benzoic acid, and (E)-4-(1-imidazolylmethyl)cinnamic acid and its α-methyl analogue showed the highest potency with an IC50 in the range of 10-8 to 10-9 M. Inhibition by these derivatives was highly selective for the TX synthetase, since other enzymes such as fatty acid cyclo-oxygenase and prostacyclin synthetase were not affected.
