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Synthesis and enzyme inhibitory activities of some new pyrazole-based heterocyclic compounds |
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| Authors: | Tariq Harit Fouad Malek Brahim El Bali Ajmal Khan Kourosh Dalvandi Bishnu P. Marasini Shagufta Noreen Rizwana Malik Sadia Khan M. Iqbal Choudhary |
| Affiliation: | 1. Laboratory of Organic Chemistry, Macromolecular and Naturals Products, URAC 25, Faculty of Sciences, University Mohamed I, P.O. Box 717, 60000, Oujda, Morocco 2. Laboratory of Mineral Solid and Analytical Chemistry, Faculty of Sciences, University Mohamed I, P.O. Box 717, 60000, Oujda, Morocco 3. HEJ Research Institute of Chemistry, Dr. Panjwani Centre for Molecular Medicine and Drug Research, International Centre for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan 4. Dr. Panjwani Centre for Molecular Medicine and Drug Research, International Centre for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan 5. Department of Chemistry, School of Sciences, King Saudi University, Riyadh, 11475, Saudi Arabia |
| Abstract: | Three tridentate N,N-bis(3,5-dimethylpyrazol-1-ylmethyl)-1-hydroxy-2-aminoethane (2), N,N-bis(3,5-dimethylpyrazol-1-ylmethyl)-cyclohexylamine (3) and 2-[bis(1,5-dimethyl-1H-pyrazol-3-ylmethyl)amino]ethan-1-ol (4) are synthesized and spectroscopically characterized together with 1-hydroxymethyl-3,5-dimethylpyrazole (1). These have been tested in inhibitory activities against various hyperactive enzymes like urease, β-glucuronidase, phosphodiesterase, α-chymotrypsin, acetylcholinesterase and butyrylcholinesterase. Compounds 1, 2 and 3 were found to be selective inhibitors of urease. Compound 4 was found to be selective inhibitor of butyrylcholinesterase. The nature of the junction between pyrazoles cycles determined the activities of these tripods. While the tripods are inactive towards urease or glucuronidase, they turn to be selective towards butyrylcholinesterase. |
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