74226-00-9Relevant academic research and scientific papers
Novel 3-dodecanoylindole-2-carboxylic acid inhibitors of cytosolic phospholipase A2
Lehr, Matthias,Klimt, Monika,Elfringhoff, Alwine Schulze
, p. 2569 - 2572 (2007/10/03)
Derivatives of 1-[2-(4-carboxyphenoxy)ethyl]-3-dodecanoylindole-2-carboxylic acid (4) with modified substituents at the indole-1-position were synthesized and evaluated for their ability to inhibit the arachidonic acid release in human platelets mediated by the cytosolic phospholipase A2. One of the most active compounds obtained was 26 with an IC50 of 0.44 μM.
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).
