Search for: [Abstract = "f HC\-030031 ˗ the model TRPA1 channel antagonist and drug\-likeness analysis in silico. The designed new compounds were obtained by multi\-step procedure, using classical chemical methods, and microwave\-assisted synthesis. In the first step, intermediate esters were obtained, followed by acids and hydrazides. In the final step, the condensation reaction with amines or aldehydes took place, respectively leading to the final N\-phenylamides \(series Ia˗Va\) and N'\-benzylidenohydrazides \(series Ib˗Vb\). The identity of the new final products and intermediates was confirmed by spectral \(1H NMR\) and for the compounds 93, 94, 97, 98, 101, 102, 105˗107, 109˗117 by elemental analysis. Molecular weights were verified by UPLC\/MS. The purity of the obtained compounds was determined using the UPLC\/MS technique. For the all 135 novel compounds, the antagonistic activity of the TRPA1 channel was determined using a fluorometric calcium imaging assay and HEK\-293 cells stably expressing human TRPA1 channel. The biological tests in vitro allowed to select from the series of tested compounds the potent TRPA1 channel antagonists, with better antagonistic activity than that of HC\-030031. Analysis of the structure\-activity relationship \(SAR\) in the search groups of 1,3\-dimethyl\-3,7\-dihydro\-1H\-purine\-2,6\-dione and 1H\-benzimidazole derivatives allowed to determine the influence of structural elements on the"]

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