Literature DB >> 24486414

Synthesis and in vitro urease inhibitory activity of N,N'-disubstituted thioureas.

Khalid Mohammed Khan1, Farzana Naz2, Muhammad Taha3, Ajmal Khan2, Shahnaz Perveen4, M I Choudhary2, Wolfgang Voelter5.   

Abstract

Thiourea derivatives (1-38) were synthesized and evaluated for their urease inhibition potential. The synthetic compounds showed a varying degree of in vitro urease inhibition with IC50 values 5.53 ± 0.02-91.50 ± 0.08 μM, most of which are superior to the standard thiourea (IC₅₀ = 21.00 ± 0.11 μM). In order to ensure the mode of inhibition of these compounds, the kinetic study of the most active compounds has been carried out. Most of these inhibitors were found to be mixed-type of inhibitors, except compounds 13 and 30 which were competitive, while compound 19 was identified as non-competitive inhibitor with Ki values between 8.6 and 19.29 μM.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  In vitro urease inhibition activity; Kinetic study; Synthesis; Thiourea derivatives

Mesh:

Substances:

Year:  2014        PMID: 24486414     DOI: 10.1016/j.ejmech.2014.01.001

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  7 in total

Review 1.  A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria.

Authors:  Yuri F Rego; Marcelo P Queiroz; Tiago O Brito; Priscila G Carvalho; Vagner T de Queiroz; Ângelo de Fátima; Fernando Macedo
Journal:  J Adv Res       Date:  2018-05-04       Impact factor: 10.479

Review 2.  A minireview on what we have learned about urease inhibitors of agricultural interest since mid-2000s.

Authors:  Luzia V Modolo; Cristiane J da-Silva; Débora S Brandão; Izabel S Chaves
Journal:  J Adv Res       Date:  2018-04-17       Impact factor: 10.479

3.  Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity.

Authors:  Mariusz Mojzych; Paweł Tarasiuk; Katarzyna Kotwica-Mojzych; Muhammad Rafiq; Sung-Yum Seo; Michał Nicewicz; Emilia Fornal
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-25       Impact factor: 5.051

4.  Profiling of phytochemicals from aerial parts of Terminalia neotaliala using LC-ESI-MS2 and determination of antioxidant and enzyme inhibition activities.

Authors:  Muhammad Nadeem Shahzad; Saeed Ahmad; Muhammad Imran Tousif; Imtiaz Ahmad; Huma Rao; Bilal Ahmad; Abdul Basit
Journal:  PLoS One       Date:  2022-03-31       Impact factor: 3.240

5.  Metabolic Profiling by GC-MS, In Vitro Biological Potential, and In Silico Molecular Docking Studies of Verbena officinalis.

Authors:  Rabia Nisar; Saeed Ahmad; Kashif-Ur-Rehman Khan; Asmaa E Sherif; Fawaz Alasmari; Afaf F Almuqati; Chitchamai Ovatlarnporn; Mohsin Abbas Khan; Muhammad Umair; Huma Rao; Bilal Ahmad Ghalloo; Umair Khurshid; Rizwana Dilshad; Khaled S Nassar; Sameh A Korma
Journal:  Molecules       Date:  2022-10-08       Impact factor: 4.927

6.  N-Aryl-3,4-dihydroisoquinoline Carbothioamide Analogues as Potential Urease Inhibitors.

Authors:  Fayaz Ali; Shahbaz Shamim; Mehreen Lateef; Khalid Mohammed Khan; Muhammad Taha; Uzma Salar; Abdul Wadood; Ashfaq Ur Rehman; Noor Ul Ain Nawaz; Shahnaz Perveen
Journal:  ACS Omega       Date:  2021-06-07

7.  Thiourea-Derived Chelating Ligands and Their Organometallic Compounds: Investigations into Their Anticancer Activity.

Authors:  Kelvin K H Tong; Muhammad Hanif; James H Lovett; Katja Hummitzsch; Hugh H Harris; Tilo Söhnel; Stephen M F Jamieson; Christian G Hartinger
Journal:  Molecules       Date:  2020-08-11       Impact factor: 4.411

  7 in total

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