737742-80-2Relevant academic research and scientific papers
Discovery of Irbesartan Derivatives as BLT2 Agonists by Virtual Screening
Hernandez-Olmos, Victor,Heering, Jan,Bischoff-Kont, Iris,Kaps, Alexander,Rajkumar, Rinusha,Liu, Ting,Fürst, Robert,Steinhilber, Dieter,Proschak, Ewgenij
, p. 1261 - 1266 (2021)
Leuktriene B4 receptor 2 (BLT2) is a G-protein coupled receptor modulation of which is discussed to be a therapeutic option for healing of intestinal lesions. In this work, new BLT2 agonists were identified by a virtual screening of a repurposing library and in vitro assay of the most promising compounds. Irbesartan, an approved type-1 angiotensin II receptor (AT1) antagonist, was identified as a moderate BLT2 agonist. An initial SAR study on the irbesartan scaffold was performed resulting in the discovery of a new potent BLT2 agonist (8f, EC50 = 67.6 nM). Irbesartan and 8f were shown to promote proliferation of epithelial colon cells, an effect which was reversible by a BLT2 antagonist.
SUBSTITUTED IMIDAZOLONE DERIVATIVES, PREPARATIONS AND USES
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Page/Page column 39, (2010/02/16)
The present invention relates to polysubstituted imidazolone derivatives, to the pharmaceutical compositions comprising them and to the therapeutic uses thereof in the human and animal health fields. The present invention also relates to a process for preparing these derivatives.
