Smart urea ionic co-crystals with enhanced urease inhibition activity for improved nitrogen cycle management

2018 ◽  
Vol 54 (55) ◽  
pp. 7637-7640 ◽  
Author(s):  
Lucia Casali ◽  
Luca Mazzei ◽  
Oleksii Shemchuk ◽  
Kenneth Honer ◽  
Fabrizia Grepioni ◽  
...  
Keyword(s):  
Soil Nutrients ◽  
Nitrogen Cycle ◽  
Urease Inhibitor ◽  
Urease Inhibition ◽  
Inhibition Activity ◽  
N Supply ◽  
Solution Methods ◽  
Urease Inhibition Activity

A smart ionic co-crystal of urea with KCl and ZnCl2, obtainedviamechanochemical and solution methods has been proven to be a very efficient urease inhibitor and to provide soil nutrients to complement N supply.

Amino acid conjugated antimicrobial drugs: Synthesis, lipophilicity- activity relationship, antibacterial and urease inhibition activity

2018 ◽  
Vol 145 ◽  
pp. 140-153 ◽  
Author(s):  
Atta Ullah ◽  
Fatima Iftikhar ◽  
Muhammad Arfan ◽  
Syeda Tayyaba Batool Kazmi ◽  
Muhammad Naveed Anjum ◽  
...  
Keyword(s):  
Amino Acid ◽  
Activity Relationship ◽  
Urease Inhibition ◽  
Inhibition Activity ◽  
Antimicrobial Drugs ◽  
Urease Inhibition Activity

scholarly journals Crystal engineering of exemestane to obtain a co-crystal with enhanced urease inhibition activity

IUCrJ ◽  
2020 ◽  
Vol 7 (1) ◽  
pp. 105-112 ◽  
Author(s):  
Syeda Saima Fatima ◽  
Rajesh Kumar ◽  
M. Iqbal Choudhary ◽  
Sammer Yousuf
Keyword(s):  
Crystal Engineering ◽  
Geometric Analysis ◽  
Biological Properties ◽  
Urease Inhibition ◽  
Inhibition Activity ◽  
Scanning Calorimetry ◽  
Pharmaceutical Ingredients ◽  
Crystal Stability ◽  
Urease Inhibition Activity

Co-crystallization is a phenomenon widely employed to enhance the physio-chemical and biological properties of active pharmaceutical ingredients (APIs). Exemestane, or 6-methylideneandrosta-1,4-diene-3,17-dione, is an anabolic steroid used as an irreversible steroidal aromatase inhibitor, which is in clinical use to treat breast cancer. The present study deals with the synthesis of co-crystals of exemestane with thiourea by liquid-assisted grinding. The purity and homogeneity of the exemestane–thiourea (1:1) co-crystal were confirmed by single-crystal X-ray diffraction followed by thermal stability analysis on the basis of differential scanning calorimetry and thermogravimetric analysis. Detailed geometric analysis of the co-crystal demonstrated that a 1:1 co-crystal stoichiometry is sustained by N—H...O hydrogen bonding between the amine (NH2) groups of thiourea and the carbonyl group of exemestane. The synthesized co-crystal exhibited potent urease inhibition activity in vitro (IC50 = 3.86 ± 0.31 µg ml−1) compared with the API (exemestane), which was found to be inactive, and the co-former (thiourea) (IC50 = 21.0 ± 1.25 µg ml−1), which is also an established tested standard for urease inhibition assays in vitro. The promising results of the present study highlight the significance of co-crystallization as a crystal engineering tool to improve the efficacy of pharmaceutical ingredients. Furthermore, the role of various hydrogen bonds in the crystal stability is successfully analysed quantitatively using Hirshfeld surface analysis.

scholarly journals Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives

2013 ◽  
Vol 78 (8) ◽  
pp. 1127-1134 ◽  
Author(s):  
Ghulam Fareed ◽  
Nighat Afza ◽  
Ali Versiani ◽  
Nazia Fareed ◽  
Rasheed Mughal ◽  
...  
Keyword(s):  
Spectroscopic Characterization ◽  
Significant Inhibition ◽  
Diffusion Method ◽  
Urease Inhibition ◽  
Inhibition Activity ◽  
Mueller Hinton ◽  
Excellent Activity ◽  
Mueller Hinton Agar ◽  
Ft Ir ◽  
Urease Inhibition Activity

A series of 4-aryl methylidene-2-phenyl/methyl-5-(4H)-oxazolone derivatives (2-7) have been synthesized using the reported method by condensation of aldehydes with N-benzoyl / N-acetyl glycine in the presence of zinc oxide as a catalyst and acetic anhydride at room temperature in ethanol. The compounds (2-6) are new derivatives. The structures of compounds were evaluated on the basis of 1H-NMR, 13C-NMR, EIMS, FT-IR and elemental analysis. All the compounds were screened for their antibacterial and urease inhibition activity. Antibacterial activity was tested by agar well diffusion method using Mueller Hinton Agar medium. Compound (2) showed excellent activity against S. aureus which has 16 mm (80%) inhibition and above 24 mm (70%) against S. typhi. The most active compound against E. coli was compound (6) having 20 mm (80%) inhibition followed by compound (5) having above 18 mm (70%) inhibition. Urease inhibition activity of all the compounds was determined by indophenol method. Compounds (3, 6) and (7) showed significant inhibition against Jacks bean urease.

A new flavanenol with urease-inhibition activity isolated from roots of manna plant camelthorn (Alhagi maurorum)

2010 ◽  
Vol 965 (1-3) ◽  
pp. 65-67 ◽  
Author(s):  
Abdul Hafeez Laghari ◽  
Shahabuddin Memon ◽  
Aisha Nelofar ◽  
Khalid M. Khan ◽  
Arfa Yasmin ◽  
...  
Keyword(s):  
Urease Inhibition ◽  
Inhibition Activity ◽  
Urease Inhibition Activity

scholarly journals Synthesis, density functional theory (DFT) studies and urease inhibition activity of chiral benzimidazoles

Heliyon ◽  
2020 ◽  
Vol 6 (10) ◽  
pp. e05187
Author(s):  
Hasil Aman ◽  
Naghmana Rashid ◽  
Zaman Ashraf ◽  
Aamna Bibi ◽  
Hsin-Tsung Chen ◽  
...  
Keyword(s):  
Density Functional Theory ◽  
Density Functional ◽  
Urease Inhibition ◽  
Dft Studies ◽  
Inhibition Activity ◽  
Functional Theory ◽  
Urease Inhibition Activity

scholarly journals Symmetrical Heterocyclic Cage Skeleton: Synthesis, Urease Inhibition Activity, Kinetic Mechanistic Insight, and Molecular Docking Analyses

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 312 ◽  
Author(s):  
Muhammad Hanif ◽  
Fariha Kanwal ◽  
Muhammad Rafiq ◽  
Mubashir Hassan ◽  
Muhammad Mustaqeem ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Competitive Inhibition ◽  
Inhibitory Effect ◽  
Urease Inhibition ◽  
Inhibition Activity ◽  
Design And Synthesis ◽  
Interactive Behavior ◽  
Ic50 Values ◽  
Urease Inhibition Activity

The present study focuses on the design and synthesis of a cage-like organic skeleton containing two triazole rings jointed via imine linkage. These molecules can act as urease inhibitors. The in-vitro urease inhibition screening results showed that the combination of the two triazole skeleton in the cage-like morphology exhibited comparable urease inhibition activity to that of the reference thiourea while the metallic complexation, especially with copper, nickel, and palladium, showed excellent activity results with IC50 values of 0.94 ± 0.13, 3.71 ± 0.61, and 7.64 ± 1.21 (3a–c), and 1.20 ± 0.52, 3.93 ± 0.45, and 12.87 ± 2.11 µM (4a–c). However, the rest of compounds among the targeted series exhibited a low to moderate enzyme inhibition potential. To better understand the compounds’ underlying mechanisms of the inhibitory effect (3a and 4a) and their most active metal complexes (3b and 4b), we performed an enzymatic kinetic analysis using the Lineweaver–Burk plot in the presence of different concentrations of inhibitors to represent the non-competitive inhibition nature of the compounds, 3a, 4a, and 4b, while mixed type inhibition was represented by the compound, 3b. Moreover, molecular docking confirmed the binding interactive behavior of 3a within the active site of the target protein.

Evaluation of Urease Inhibition Activity of Zerumbone in vitro

2017 ◽  
Vol 45 (3) ◽  
pp. 265-270 ◽  
Author(s):  
Hyun Jun Woo ◽  
Min Ho Lee ◽  
Ji Yeong Yang ◽  
Hye Jin Kwon ◽  
Min Ji Yeon ◽  
...  
Keyword(s):  
Urease Inhibition ◽  
Inhibition Activity ◽  
Urease Inhibition Activity

scholarly journals Microwave-assisted solvent free efficient synthesis of 1,3,4-oxadiazole-2(3H)-thiones and their potent in vitro urease inhibition activity

2012 ◽  
Vol 3 (2) ◽  
pp. 143-146 ◽  
Author(s):  
Sohail Anjum Shahzada ◽  
Muhammad Yar ◽  
Zulfiqar Ali Khan ◽  
Islam Ullah Khan ◽  
Syed Ali Raza Naqvi ◽  
...  
Keyword(s):  
Solvent Free ◽  
Urease Inhibition ◽  
Inhibition Activity ◽  
Efficient Synthesis ◽  
Microwave Assisted ◽  
Urease Inhibition Activity
Sign in / Sign up

Export Citation Format

Share Document