In the present work we reported the synthesis of Schiff bases from 4-phenoxy-5-sulfamoylbenzoic acid motif. The reaction was carried out by substitution of different aldehyde and ketones at sulfamoyl group of sulfamoylbenzoic acid. The generated substituted products (4a-4i) possessed potent structure activity relationship and exhibited drug like properties. The structures of synthesized compounds were characterized on the basis of FT-IR, 1H NMR, 13C NMR and mass spectroscopic data. The effects of synthesized products were investigated on urease enzyme through anti-urease enzyme inhibition assay (Weather burn method). These compounds were further evaluated for anti-bacterial potential. The Rationale behind the assessment of antibacterial activity was to investigate the synthesized compound's dual mode action against urease and virulent bacterial strains in order to develop a lead candidate for the treatment of GIT diseases such as gastric and peptic ulcers, as well as hepatic encephalopathy. The synthesized compounds have outstanding anti-urease and anti-bacterial action, as is evident from in vitro and in silico studies. As a result, these compounds (3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid; 4a-4i) might be explored further as a potential lead for the development of potent inhibitors in the future.
Synthesis, Biochemical Characterization and In-Silico Investigation of 3-(Butylamino)-4-Phenoxy-5-Sulfamoylbenzoic Acid Derivatives: Dual Action Mode Inhibitors of Urease and Virulent Bacterial Stains
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Sajid Irshad, Saeed Ahmad, Shafi Ullah Khan, Mohsin Abbas khan, Syeda Abida Ejaz, Huma Rao, Umair Khurshid, Aftab Ahmed, Nadeem Shahzad, Hamad M.Al-kahtani, Affan Waheed, Tanveer A.Wani, Abdullahi Tunde Aborode; Synthesis, Biochemical Characterization and In-Silico Investigation of 3-(Butylamino)-4-Phenoxy-5-Sulfamoylbenzoic Acid Derivatives: Dual Action Mode Inhibitors of Urease and Virulent Bacterial Stains. Biochem J 2022; BCJ20220395. doi: https://doi.org/10.1042/BCJ20220395
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