Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents |
| |
| Institution: | 1. Department of Chemistry, Hazara University, Mansehra 21120, Pakistan;2. Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia;3. Faculty of Applied Science, Universiti Teknologi MARA, 40450 Shah Alam, Malaysia;4. Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan;5. Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;6. HEJ, Research Institute of Chemistry, ICCBS, University of Karachi, Karachi 75270, Pakistan;1. School of Chemistry, The University of Manchester, Oxford Road, Manchester M13 9PL, United Kingdom;2. Manchester Institute of Biotechnology, The University of Manchester, 131 Princess Street, Manchester M1 7DN, United Kingdom;3. Natural and Medical Sciences Research Center, University of Nizwa, P.O Box 33, Postal Code 616, Birkat Al Mauz, Nizwa, Oman;4. Department of Chemistry, Quaid-i-Azam University-45320, Islamabad, Pakistan;5. Department of Chemistry, Abbottabad University of Science and Technology, Havelian, Abbottabad, Pakistan;6. Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany;1. Department of Chemistry, Hazara University, Mansehra 21300, Pakistan;2. Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;3. Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan;4. Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar, Puncak Alam, Selangor D. E, Malaysia;5. Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar, Puncak Alam, Selangor Darul Ehsan, Malaysia;6. College of Computer Science & Information Technology (CCSIT), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 3144, Saudi Arabia;7. Department of Pharmacy, University of Malakand, Chakdara, Dir (L), Khyber-Pakhtunkhwa (KPK) 18000, Pakistan;8. Department of Pharmacy, Sarhad University of Science & Information Technology, Peshawar, Pakistan;1. Department of Pharmaceutical Organic Chemistry, Beni Suef University, Beni Suef 62514, Egypt;2. Pharmaceutical Chemistry Department, College of Pharmacy, Al Jouf University, Sakaka, Al Jouf 2014, Saudi Arabia;1. Key Laboratory of Marine Pharmaceutical Compound Screening, Huaihai Institute of Technology, Lianyungang, 222005, People''s Republic of China;2. Pharmacy School, Huaihai Institute of Technology, Lianyungang, 222005, People''s Republic of China;3. Co-Innovation Center of Jiangsu Marine Bio-industry Technology, Lianyungang, 222005, People''s Republic of China;1. Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 31441, Dammam, Saudi Arabia;2. Depatment of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan;3. Monash University School of Chemical Engineering, Bandar Sunway 47500 Selangor Darul Ehsan, Malaysia;4. Department of Chemistry, University of Karachi, Karachi 75270, Pakistan;5. Department of Neuroscience Research, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;6. Department of Nano-Medicine Research, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;7. Department of Biochemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan;8. Department of Chemistry, University of Wah, Quaid Avenue, Wah Cantt 47000, Pakistan;9. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;1. Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Ghal Kalan, Moga, Punjab 142001, India;2. GRT Institute of Pharmaceutical Education and Research, GRT Mahalakshmi Nagar, Tiruttani, India;3. Amity Institute of Pharmacy, Amity University Uttar Pradesh, Lucknow Campus, India;4. College of Pharmacy and Health Sciences, University of Science and Technology of Fujairah, United Arab Emirates |
| |
| Abstract: | 4-Thiazolidinone analogs 1–20 were synthesized, characterized by 1H NMR and EI–MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73–69.65 μM, if compared with standard thiourea having IC50 value of 21.25 ± 0.15 μM. Among the series, eight derivatives 3, 6, 8, 10, 15, 17, 19, and 20 showed outstanding urease inhibitory potential with IC50 values of 9.34 ± 0.02, 14.62 ± 0.03, 8.43 ± 0.01, 7.3 ± 0.04, 2.31 ± 0.002, 5.75 ± 0.003, 8.81 ± 0.005, and 1.73 ± 0.001 μM, respectively, which is better than the standard thiourea. The remaining analogs showed good to excellent urease inhibition. The binding interactions of these compounds were confirmed through molecular docking studies. |
| |
| Keywords: | 4-Thiazolidinone Synthesis Urease inhibition Docking studies |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
