30170-83-3Relevant academic research and scientific papers
1-[(Aryloxy)alkyl]-1H-imidazoles as inhibitors of neuronal nitric oxide synthase
Salerno,Sorrenti,Guerrera,Sarva,Siracusa,Di Giacomo,Vanella
, p. 491 - 494 (1999)
A series of 1-[(aryloxy)alkyl]-1 H-imidazoles were synthesized from imidazole and various (aryloxy)alkyl bromides and tested for inhibitory activity against the three isoforms of nitric oxide synthase. 1-[2-(4-Bromophenoxy)ethyl]-1 H-imidazole and 1-[2-[4-(trifluoromethyl)phenoxy]ethyl]-1H-imidazole showed inhibitory activity against the neuronal isoform but were less potent against the endothelial isoform. Thus they could be considered interesting for their selectivity. The remaining compounds had only modest activity.
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).
