Fazal Habib (HEJ Research Institute of Chemistry, ICCBS, University of Karachi, Pakistan)
LinkedIn: Fazal Habib
Abstract: In organic chemistry, aromatic amines are compounds that contain an aromatic ring bonded to an amine group. They have a broad spectrum of applications across various industries, including pharmaceuticals, agrochemicals, and in the synthesis of diverse heterocyclic compounds. Heterocyclic compounds are characterized by rings that contain one or more heteroatoms, and they possess significant chemical and biological relevance. Among these, tetrahydro thiadiazine thiones (THTT) derivatives exhibit a wide spectrum of biological activities. They serve as precursor in drug delivery systems and demonstrate exceptional potential as structural units in the synthesis of novel drugs, agrochemicals, and functional materials owing to their combined lipophilic and hydrophilic properties. The synthesis of THTT derivatives was carried out by treating different alkyl/aryl amines with carbon disulfide in potassium hydroxide medium at room temperature. This was followed by the addition of
formaldehyde and a buffer solution containing 4-aminobenzoic acid, resulting in the formation of the corresponding THTT derivatives. These compounds were then refluxed in ethanol in the presence of sulfuric acid to obtain esterified THTT derivatives. The reaction progress was monitored by thin layer chromatography. Structural confirmation of the synthesized compounds was confirmed using proton nuclear magnetic resonance spectroscopy. The in vitro inhibition activities of the synthesized compounds were evaluated against α-amylase and urease enzymes. Among the tested compounds, F7 exhibited the lowest, F4 shows the highest, while the remaining six compounds demonstrated moderate αamylase and urease inhibitory activities.
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