The work reports synthesis of ten novel derivatives of 5-(1-(substituted phenyl)-4,5-diphenyl-1H-imidazol-2-yl)-4-methylthiazole 5(a-o). The reaction of benzil, primary aryl amines, 4-methylthiazole-5-carbaldehyde, and ammonium acetate was carried out in one pot in presence of eco-friendly catalyst cerric ammonium nitrate in solvent ethanol to give final compounds. The synthesized derivatives were evaluated for their in vitro antifungal activity against pathogenic fungal stains. Molecular modelling studies suggested that some of the synthesized derivatives, especially 5b and 5c exhibited excellent antifungal activity whereas all imidazole derivatives 5(a-o) have potential to explore in the drug discovery pipeline for antifungal agents. The structures of the synthesized compounds were confirmed by spectral characterization such as IR, 1H NMR, 13CNMR and Mass spectral studies. In addition to this the in silico ADMET study, was also performed which proves that the synthesized compounds exhibit good oral absorption and are non- toxic in nature.
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Ultrasound-Assisted One Pot CAN catalyze synthesis and antifungal evaluation of Novel 5-(1-(substituted phenyl)-4, 5-diphenyl-1H-imidazol-2-yl)-4-methylthiazole
Published: 14 November 2018 by MDPI in The 22nd International Electronic Conference on Synthetic Organic Chemistry session General Organic Synthesis
Keywords: Thiazolyl imidazole, multicomponent synthesis, CAN, Ultra-sonication, Antifungal activity.