Identification of novel quinazolin-4(3H)-ones as inhibitors of thermolysin,the prototype of the M4 family of proteinases |
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| Authors: | Mahmud Tareq Hassan Khan Rasool Khan Yimingjiang Wuxiuer Mohammad Arfan Manzoor Ahmed Ingebrigt Sylte |
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| Institution: | 1. Medical Pharmacology and Toxicology, Department of Medical Biology, Faculty of Health Science, University of Tromsø, N-9037 Tromsø, Norway;2. Department of Chemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan;3. Institute of Chemical Sciences, University of Peshawar, Peshawar 25120, Pakistan;4. Department of Chemistry, University of Malakand, Chakdara, N.W.F.P., Pakistan |
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| Abstract: | A combinatorial series of novel quinazolin-4(3H)-ones were synthesised and their structures were established based on spectroscopic data (IR, NMR, EI-MS, and FAB-MS). The compounds were tested for inhibition of the zinc metalloproteinase thermolysin (TLN) utilizing a chemical array-based approach. Some of the compounds were found to inhibit TLN, with IC50 values ranging from 0.0115 μM (compound 3) to 122,637 μM (compound 29). Compound 3 3-phenyl-2-(trifluoromethyl) quinazolin-4(3H)-one] (IC50 = 0.0115 μM) and compound 35 3-(isopropylideneamino)-2,2-dimethyl-2,3-dihydroquinazolin-4 (1H)-one] (IC50 = 0.2477 μM) were found to be the most potent inhibitors. |
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