512796-24-6Relevant articles and documents
Novel N-Cycloalkylcarbonyl-N′-arylthioureas: Synthesis, Design, Antifungal Activity and Gene Toxicity
Kholodniak, Olena V.,Kazunin, Maksym S.,Meyer, Fatuma,Kovalenko, Sergiy I.,Steffens, Karl G.
, (2020)
A synthesis method of novel N-cycloalkylcarbonyl-N′-arylthioureas was developed. It consists of sequential addition of equimolecular amounts of ammonium isothiocyanate and substituted anilines to cycloalkylcarbonyl chlorides. The identity and purity of products were confirmed by LC/MS spectra, their structure by elemental analysis, IR and 1H-NMR spectra. Preliminary antimicrobial screening for standard microorganisms and molecular docking allowed to select several structures for antifungal and genetic toxicity studies. Conducted in vitro screening of 9 compounds for antifungal potential against 11 phytopathogenic fungi and three Phytophthora strains revealed that two N-(arylcarbamothioyl) cyclopropanecarboxamides at a concentration of 50 μg/ml exhibited activities comparable to the standard antifungal agent ‘Cyproconazole’. Analysis of mutagenicity of novel thioureas using the Salmonella reverse mutagenicity assay (‘Ames Test’) showed a low gene-toxicity profile.