| Literature DB >> 26520885 |
Fazal Rahim1, Khalid Zaman2, Hayat Ullah2, Muhammad Taha3, Abdul Wadood4, Muhammad Tariq Javed2, Wajid Rehman2, Muhammad Ashraf5, Reaz Uddin6, Imad Uddin2, Humna Asghar5, Aftab Ahmad Khan2, Khalid M Khan6.
Abstract
4-Thiazolidinone analogs 1-20 were synthesized, characterized by (1)H NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65μM, if compared with standard thiourea having IC50 value of 21.25±0.15μM. 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±0.001μM, 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.Entities:
Keywords: 4-Thiazolidinone; Docking studies; Synthesis; Urease inhibition
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Year: 2015 PMID： 26520885 DOI： 10.1016/j.bioorg.2015.10.005
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275