Novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one derivatives as potential inhibitors of chorismate mutase |
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| Institution: | 1. Center for Pharmaceutical Sciences, Institute of Science and Technology, Jawaharlal Nehru Technological University, Hyderabad 500 085, Andhra Pradesh, India;2. Custom Pharmaceutical Services, Dr. Reddy’s Laboratories Limited, Bollaram Road Miyapur, Hyderabad 500 049, India;3. Dr Reddy’s Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India;4. Doctoral Program in Experimental Biology and Biomedicine, Center for Neuroscience and Cell Biology, University of Coimbra, Portugal;1. Department of Interventional Therapy, Department of Rehabilitation, Dalian Municipal Central Hospital, Dalian 116033, P.R. China;2. Department of Anesthesiology, First Affiliated Hospital, Dalian Medical University, Dalian 116011, P.R. China;3. Department of Engineering, St. Cross College, University of Oxford, Oxford, OX1 3LZ, UK;4. School of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian 116600, P.R. China;1. Department of Chemistry, Hazara University, Mansehra 21120, Pakistan;2. Department of Pharmacology, Rawalpindi Medical University, Rawalpindi 463000, Pakistan;3. Department of Pharmacy, University of Malakand, Chakdara 18000, Dir (L), Pakistan;4. Department of Chemistry, COMSATS University Islamabad, Abbottabad Campus 22060, Pakistan;5. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;6. Department of Biotechnology, University of Azad Jammu & Kashmir Bagh, Pakistan;7. Department of Chemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan;1. Department of Chemistry, Hazara University, Mansehra 21120, Pakistan;2. Department of Pharmacy, University of Malakand, Chakdara, 18000 Dir (L), Pakistan;3. Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan;1. Discovery Sciences, Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, United States;2. Cardiovascular & Metabolic Research, Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, United States;1. Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan;2. Faculty of Chemistry, University of Warsaw, Pasteura 1, 02-093 Warsaw, Poland;3. Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland;4. Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan;5. Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;6. Department of Biochemistry & Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;7. Department of Chemistry, GC University, Lahore 54000, Pakistan |
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| Abstract: | A series of novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives were designed, synthesized and evaluated in vitro as potential inhibitors of chorismate mutase (CM). All these compounds were prepared via a multi-component reaction (MCR) involving sequential I2-mediated Biginelli reaction followed by Cu-free Sonogashira coupling. Some of them showed promising inhibitory activities when tested at 30 μM. One compound showed dose dependent inhibition of CM with IC50 value of 14.76 ± 0.54 μM indicating o-alkynylphenyl substituted DHPM as a new scaffold for the discovery of promising inhibitors of CM. |
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| Keywords: | Pyrimidinone Alkyne Iodine Palladium Chorismate mutase |
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