75912-91-3Relevant academic research and scientific papers
N-(phenoxyalkyl)imidazoles as selective inhibitors of the thromboxane synthetase enzyme and pharmaceutical compositions thereof
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, (2008/06/13)
N-(mono or disubstituted phenoxyalkyl)imidazoles and the pharmaceutically acceptable acid addition salts thereof are able to selectively inhibit the action of the thromboxane synthetase enzyme without significantly inhibiting the action of the prostacycline synthetase or cyclooxygenase enzymes and are thus useful in the treatment of ischaemic heart disease, stroke, transient ischaemic attack, thrombosis, migraine, and the vascular complications of diabetes.
Selective Thromboxane Synthetase Inhibitors. 1. 1--1H-imidazoles
Cross, Peter E.,Dickinson, Roger P.,Parry, M. John,Randall, Michael J.
, p. 1427 - 1432 (2007/10/02)
1-(2-Phenoxyethyl)-1H-imidazole was found to be an inhibitor of thromboxane (TxA2) synthetase, but it also inhibited the adrenal cytochrome P-450 enzyme steroid 11β-hydroxylase.The preparation of a series of analogues is described, and activity against TxA2 synthetase, PGI2 synthetase, cyclooxygenase, and steroid 11β-hydroxylase is discussed.Potency against TxA2 synthetase was increased by introduction of a carboxyl group at a suitable distance from the imidazole ring.A distance of 8.1-8.8 Angstroem between N-1 of the imidazole and the carboxyl carbon was found to be optimal.Introduction of a carboxyl group also had the effect of reducing activity against steroid 11β-hydroxylase.The most potent and selective compound was found to be 4-benzoic acid (14).
