New 1-octanoyl-3-aryl thiourea derivatives: Solvent-free synthesis, characterization and multi-target biological activities

Abstract

<p>An efficient solvent-free synthesis of a 10-member library of octanoyl linked substituted aryl thioureas was accomplished successfully. The octanoyl isothiocyanate was freshly prepared in excellent yield and purity by the reaction of potassium thiocyanate with octanoyl chloride followed by removal of potassium chloride by filtration. The reaction of the latter with a series of ten different substituted anilines by stirring at 60-65°C lead to the formation of the title compounds. The <em>in vitro</em> antifungal activity of newly synthesized compounds was evaluated against <em>Aspergillus niger, A. flavus</em> and <em>Fusarium solani</em> strains of pathogenic fungi. Antibacterial assay was carried out against Gram positive (<em>Staphylococcus aureus, Micrococcus luteus</em>) and Gram negative bacterial strains (<em>Escherichia coli, Enterobacter aerogens</em>). Furthermore, anti-oxidant potential and enzyme inhibition studies against α-amylase and butyryl cholinestrase were performed. The results obtained indicated moderate to excellent activities of most of the compounds whilst some derivatives showed potency higher than the standard used.</p><p><strong>Video Clips</strong>:</p><p><a href="https://www.youtube.com/v/GJ8JFPUHdo4">Antibacterial assay</a>: 2 min 16 sec</p><p><a href="https://www.youtube.com/v/1j73_wjZaOE">Enzyme inhibition</a>: 1 min 27 sec </p>

Jack Bean Urease Inhibitors, and Antioxidant Activity Based on Palmitic acid Derived 1-acyl-3- Arylthioureas: Synthesis, Kinetic Mechanism and Molecular Docking Studies

“…Radical scavenging activity was determined by modifying already reported method by 2, 2-diphenyl-1 picrylhydrazyl (DPPH) assay [24]. The assay solution consisted of 100 µL of DPPH (150 µM), 20 µL of increasing concentration of test compounds and the volume was adjusted to 200 µL in each well with DMSO.…”

“…Thioureas are the versatile organosulfur small-molecules capable of showing applications in all fields like agriculture, environ-ment, medicine, cosmetics, industrial, and material chemistry [13][14][15][16][17][18][19][20]. Acylthioureas serve as key precursors in the synthesis of metal complexes and also serve as valuable synthon in the synthesis wide variety of heterocyclic motifs [21][22][23][24][25].…”

Hybrid Pharmacophoric Approach in the Design and Synthesis of Coumarin Linked Pyrazolinyl as Urease Inhibitors, Kinetic Mechanism and Molecular Docking

“…Helicobacter pylori is lethal for human health as it causes the numerous stomach related disorders such as pyelonephritis, hepatic coma, peptic ulcer, and formation of kidney stones. Moreover, urease enzyme is also responsible for the decline in crop production because it deprives of the soil from an essential fertilizer urea by releasing harmful gases which may lead to global warming …”

An expedient synthesis of N‐(1‐(5‐mercapto‐4‐((substituted benzylidene)amino)‐4H‐1,2,4‐triazol‐3‐yl)‐2‐phenylethyl)benzamides as jack bean urease inhibitors and free radical scavengers: Kinetic mechanism and molecular docking studies

“…1,2,4‐Triazole moiety represents the major pharmacophore, possessing a wide range of biological activities. [17,18] Similarly, hydrazone compounds possessing hydrazine moiety –NHN=CH‐ constitute an important class of compounds for new drug development . These ligands play an important role in the development of co‐ordination chemistry.…”