| Literature DB >> 34361659 |
Faizan Ur Rahman1, Maryam Bibi2, Ezzat Khan1,2, Abdul Bari Shah3, Mian Muhammad1, Muhammad Nawaz Tahir4, Adnan Shahzad5, Farhat Ullah6, Muhammad Zahoor7, Salman Alamery8, Gaber El-Saber Batiha9.
Abstract
In this study six unsymmetrical thiourea derivatives, 1-isobutyl-3-cyclohexylthiourea (1), 1-tert-butyl-3-cyclohexylthiourea (2), 1-(3-chlorophenyl)-3-cyclohexylthiourea (3), 1-(1,1-dibutyl)-3-phenylthiourea (4), 1-(2-chlorophenyl)-3-phenylthiourea (5) and 1-(4-chlorophenyl)-3-phenylthiourea (6) were obtained in the laboratory under aerobic conditions. Compounds 3 and 4 are crystalline and their structure was determined for their single crystal. Compounds 3 is monoclinic system with space group P21/n while compound 4 is trigonal, space group R3:H. Compounds (1-6) were tested for their anti-cholinesterase activity against acetylcholinesterase and butyrylcholinesterase (hereafter abbreviated as, AChE and BChE, respectively). Potentials (all compounds) as sensing probes for determination of deadly toxic metal (mercury) using spectrofluorimetric technique were also investigated. Compound 3 exhibited better enzyme inhibition IC50 values of 50, and 60 µg/mL against AChE and BChE with docking score of -10.01, and -8.04 kJ/mol, respectively. The compound also showed moderate sensitivity during fluorescence studies.Entities:
Keywords: X-ray structure; docking studies; enzyme inhibition; mercury sensing; thiourea derivatives
Year: 2021 PMID: 34361659 DOI: 10.3390/molecules26154506
Source DB: PubMed Journal: Molecules ISSN: 1420-3049 Impact factor: 4.411