By a News Reporter-Staff News Editor at Life Science Weekly -- Investigators publish new report on Enzymes and Coenzymes. According to news reporting out of Abbottabad, Pakistan, by NewsRx editors, research stated, "A variety of 1-substituted-3-(3-aminosulfonylphenyl)thioureas (3a-k) and two new 1-aroyl-3-(4-aminosulfonylphenyl)thiourea derivatives (5a and 5b) were synthesized by reaction of 3-aminobenzenesulfonamide and 4-aminobenzenesulfonamide respectively with freshly prepared aroyl/heteroaryl isothiocyanates in dry acetonitrile. FTIR, H-1 NMR, C-13 NMR, GC-MS and elemental analyses data confirmed the assigned structures to the synthesized compounds."
Our news journalists obtained a quote from the research from the COMSATS Institute of Information Technology, "Further structure of compound (3g) was also confirmed by single crystal XRD analysis. The compounds were investigated as inhibitors of the bovine erythrocyte carbonic anhydrase isoform II (bCA II). The inhibition constants of these compounds against bCA II were in the range 0.011-17.1 mu M. Among the evaluated compounds, 1-substituted -3-(3-aminosulfonylphenyl)thiourea derivatives 3h and 5a were the most potent inhibitors with IC50 of 0.052 and 0.011 mu M, respectively."
According to the news editors, the research concluded: "In silico docking and molecular dynamics simulation studies were performed against bCA II and human CA II enzymes to rationalize the inhibitory properties of these compounds."
For more information on this research see: New aminobenzenesulfonamide-thiourea conjugates: Synthesis and carbonic anhydrase inhibition and docking studies. European Journal of Medicinal Chemistry, 2014;78():140-150. European Journal of Medicinal Chemistry can be contacted at: Elsevier France-Editions Scientifiques Medicales Elsevier, 23 Rue Linois, 75724 Paris, France. (Elsevier - www.elsevier.com; European Journal of Medicinal Chemistry - www.elsevier.com/wps/product/cws_home/505813)
Our news journalists report that additional information may be obtained by contacting S. Zaib, COMSATS Inst Informat Technol, Dept. of Pharmaceut Sci, Abbottabad 22060, Pakistan. Additional authors for this research include A. Saeed, K. Stolte, U. Florke, M. Shahid and J. Iqbal (see also Enzymes and Coenzymes).
Keywords for this news article include: Asia, Pakistan, Abbottabad, Hydro-Lyases, Carbonic Anhydrases, Enzymes and Coenzymes
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