779309-80-7Relevant articles and documents
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
supporting information, p. 1261 - 1266 (2021/07/28)
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.
Synthetic method of imidazolinone derivative
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Paragraph 0069-0076, (2021/07/10)
The invention discloses a synthesis method of an imidazolinone derivative. According to the method, amidine compounds and polyhydric alcohol compounds are taken as raw materials, high-value conversion of polyhydric alcohol is catalyzed by a cobalt catalyst to form a series of imidazolinone derivatives, a novel and green synthesis path meeting the sustainable chemical principle is developed, high-value conversion of renewable resources is achieved, and the method is suitable for industrial production. Therefore, the synthesis requirements on the imidazolinone derivative are met. The synthesis method has the advantages of wide substrate applicability, good functional group compatibility and use of a reusable cheap metal catalyst and air as an oxidant, has potential to prepare the imidazolinone derivative in one step on a large scale, and also provides an important way for converting biomass resources into high-value functional molecules.
Efficient 4,5-dihydro-1H-imidazol-5-one formation from amidines and ketones under transition-metal free conditions?
Xie, Yanjun,Cheng, Xiufang,Liu, Saiwen,Chen, Hui,Zhou, Wang,Yang, Luo,Deng, Guo-Jun
supporting information, p. 209 - 213 (2018/04/16)
An efficient procedure for 4,5-dihydro-1H-imidazol-5-one preparation from aryl amidines and ketones under transition-metal free conditions is described. When cyclic ketones were employed, various spiro-fused 4,5-dihydro-1H-imidazol-5-ones were formed in h