A combinatorial approach for the discovery of drug-like inhibitors of 15-lipoxygenase-1 was written by van der Vlag, Ramon;Guo, Hao;Hapko, Uladzislau;Eleftheriadis, Nikolaos;Monjas, Leticia;Dekker, Frank J.;Hirsch, Anna K. H.. And the article was included in European Journal of Medicinal Chemistry in 2019.Application of 763-69-9 The following contents are mentioned in the article:
Human 15-lipoxygenase-1 (15-LOX-1) is a mammalian lipoxygenase which plays an important regulatory role in several CNS and inflammatory lung diseases. To further explore the role of this enzyme in drug discovery, novel potent inhibitors with favorable physicochem. properties are required. In order to identify such new inhibitors, we established a combinatorial screening method based on acylhydrazone chem. This represents a novel application of combinatorial chem. focusing on the improvement of physicochem. properties, rather than on potency. This strategy allowed us to efficiently screen 44 reaction mixtures of different hydrazides and our previously reported indole aldehyde core structure, without the need for individual synthesis of all possible combinations of building blocks. Our approach afforded three new inhibitors with IC50 values in the nanomolar range and improved lipophilic ligand efficiency. This study involved multiple reactions and reactants, such as Ethyl 3-ethoxypropanoate (cas: 763-69-9Application of 763-69-9).
Ethyl 3-ethoxypropanoate (cas: 763-69-9) belongs to esters. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Liquid esters of low volatility serve as softening agents for resins and plastics. Esters also include many industrially important polymers. Polymethyl methacrylate is a glass substitute sold under the names Lucite and Plexiglas; polyethylene terephthalate is used as a film (Mylar) and as textile fibres sold as Terylene, Fortrel, and Dacron.Application of 763-69-9
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