Synthesis,biological evaluation and molecular docking of novel pyrazole derivatives as potent carbonic anhydrase and acetylcholinesterase inhibitors |
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| Institution: | 1. Health Services Vocational School, Igdır University, 76000 Igdır, Turkey;2. Department of Science, Faculty of Education, Muş Alparslan University, 49250 Muş, Turkey;3. Department of Chemistry, Faculty of Science, Ataturk University, 25240 Erzurum, Turkey;4. Department of Molecular Biology and Genetics, Faculty of Arts and Science, Kilis 7 Aralik University, 79000 Kilis, Turkey;1. Department of Chemistry, Faculty of Arts and Sciences, Inönü University, 44280 Malatya, Turkey;2. Dokuz Eylül University, Faculty of Science, Department of Physics, 35160 Buca, İzmir, Turkey;3. Central Research and Applications Laboratory, Agri Ibrahim Cecen University, 04100 Agri, Turkey;4. Department of Chemistry, Faculty of Sciences, Ataturk University, 25240 Erzurum, Turkey;5. Department of Biotechnology, Faculty of Science, Bartin University, 74100 Bartin, Turkey;6. Department of Pharmacy Services, Nihat Delibalta Göle Vocational High School, Ardahan University, 75700 Ardahan, Turkey;1. Cairo University, Faculty of Pharmacy, Pharmaceutical Organic Chemistry Department, Cairo, Egypt;2. October 6 University (O6U), Faculty of Pharmacy, Pharmaceutical Organic Chemistry Department, 6th of October City, Giza, Egypt;3. Al-Azhar University, Faculty of Pharmacy, Organic Chemistry Department (Girls), Cairo, Egypt;4. Misr University for Science and Technology, Faculty of Pharmacy, Organic Chemistry Department, Giza, Egypt;5. Modern University for Technology and Information, Faculty of Pharmacy, Organic Chemistry Department, Cairo, Egypt;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey;2. Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey;3. Department of Pharmacy Services, Nihat Delibalta Göle Vocational High School, Ardahan University, 75700 Ardahan, Turkey;4. Department of Toxicology, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey;5. Open Education Faculty, Anadolu University, 26470 Eskişehir, Turkey;6. Department of Biochemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey;1. Università degli Studi di Firenze, Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via U. Schiff 6, 50019 Sesto Fiorentino, Florence, Italy;2. Istituto di Bioscienze e Biorisorse, CNR, Via Pietro Castellino 111, 80131 Napoli, Italy;3. Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia;4. Department of Chemistry, King Faisal University, Alahsa, Saudi Arabia;5. School of Chemistry, University of New South Wales, Sydney, New South Wales 2052, Australia;1. Sakarya University, Faculty of Science and Arts, Department of Chemistry, 54187 Serdivan Sakarya, Turkey;2. Department of Chemistry, Faculty of Science, Atatürk University, 25240 Erzurum, Turkey;3. Sakarya University, Faculty of Medicine, Infectious Diseases and Clinical Microbiology Department, 54290 Adapazarı Sakarya, Turkey;1. Department of Chemistry, Faculty of Science and Art, Adiyaman University, 02040 Adıyaman, Turkey;2. Department of Chemistry, Faculty of Sciences, Ataturk University, 25240 Erzurum, Turkey;3. Agri Ibrahim Cecen University, Central Research and Application Laboratory, 04100 Agri, Turkey;4. Department of Molecular Biology and Genetics, Faculty of Arts and Science, Kilis 7 Aralik University, 79000 Kilis, Turkey;5. Advanced Technology Application and Research Center, Kilis 7 Aralik University, 79000 Kilis, Turkey;6. Department of Chemistry, Faculty of Art and Science, Inonu University, 44260 Malatya, Turkey |
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| Abstract: | A series of substituted pyrazole compounds (1–8 and 9a, b) were synthesized and their structure was characterized by IR, NMR, and Mass analysis. These obtained novel pyrazole derivatives (1–8 and 9a, b) were emerged as effective inhibitors of the cytosolic carbonic anhydrase I and II isoforms (hCA I and II) and acetylcholinesterase (AChE) enzymes with Ki values in the range of 1.03 ± 0.23–22.65 ± 5.36 µM for hCA I, 1.82 ± 0.30–27.94 ± 4.74 µM for hCA II, and 48.94 ± 9.63–116.05 ± 14.95 µM for AChE, respectively. Docking studies were performed for the most active compounds, 2 and 5, and binding mode between the compounds and the receptors were determined. |
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| Keywords: | Substituted pyrazole Acetylcholinesterase Carbonic anhydrase Enzyme inhibition |
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