urease inhibitory
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Author(s):  
Mahmoud N. M. Yousif ◽  
Abdel-Rahman B. A. El-Gazzar ◽  
Hend N. Hafez ◽  
Ahmed A. Fayed ◽  
Ahmed ElRashedy ◽  
...  

Abstract: This review describes different synthetic methods for the preparation of sulfonamides. Generally, sulfonamides are synthesized from sulfonyl chloride derivative and amino derivative. A series of sulfonamide derivatives 7a-c, 8a,b, 9, 10, 11a,b, 12 were synthesized in alkaline media by reaction of different amino compounds with p-toluene sulfonyl chloride. Different amino derivatives 13, 15, 17, 19, 21 react with p-tolyl sulphonylchloride to afford sulfonylamides 14, 16, 18, 20, 22. Different reactions of sulfonamide derivatives have been summarized. Generally, sulfonamide function group does not take part in any reactions, but there are other functional groups in the compound which make the reactions. Sulfonamides have different biological activities e.g. antibacterial activity, anticancer activity, urease inhibitory activity, radical scavenging activity, carbonic anhydrase inhibitor, non-competitive inhibitor of lactoperoxidase, antifungal activity, and anti-mycobacterial activity.


2021 ◽  
Vol 68 (4) ◽  
pp. 961-969
Author(s):  
Shuang Han ◽  
Yuan Wang

Urease inhibitors can inhibit the decomposition rate of urea, and decrease the air pollution caused by ammonia. In this paper, four new copper(II) complexes [CuL(ONO2)]n (1), [Cu2L2(μ1,3-N3)2] (2), [CuBrL] (3), and [CuClL] (4), where L = 5-bromo-2-(((2-methylamino)ethyl)imino)methyl)phenolate, have been synthesized and characterized. The complexes were characterized by elemental analyses, IR and UV-Vis spectroscopy, molar conductivity, and single crystal X-ray diffraction. X-ray analysis reveals that Cu atoms in complexes 1 and 2 are in square pyramidal coordination, and those in complexes 3 and 4 are in square planar coordination. The molecules of the complexes are linked through hydrogen bonds and π···π interactions. The inhibitory effects of the complexes on Jack bean urease were studied, which showed that the complexes have effective activity on urease.


2021 ◽  
pp. 105545
Author(s):  
Sumera Zaib ◽  
Muhammad Tayyab Younas ◽  
Seyed-Omar Zaraei ◽  
Imtiaz Khan ◽  
Hanan S. Anbar ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6658
Author(s):  
Ishani P. Kalatuwawege ◽  
Medha J. Gunaratna ◽  
Dinusha N. Udukala

Gastrointestinal tract infection caused by Helicobacter pylori is a common virulent disease found worldwide, and the infection rate is much higher in developing countries than in developed ones. In the pathogenesis of H. pylori in the gastrointestinal tract, the secretion of the urease enzyme plays a major role. Therefore, inhibition of urease is a better approach against H. pylori infection. In the present study, a series of syn and anti isomers of N-substituted indole-3-carbaldehyde oxime derivatives was synthesized via Schiff base reaction of appropriate carbaldehyde derivatives with hydroxylamine hydrochloride. The in vitro urease inhibitory activities of those derivatives were evaluated against that of Macrotyloma uniflorum urease using the modified Berthelot reaction. Out of the tested compounds, compound 8 (IC50 = 0.0516 ± 0.0035 mM) and compound 9 (IC50 = 0.0345 ± 0.0008 mM) were identified as the derivatives with potent urease inhibitory activity with compared to thiourea (IC50 = 0.2387 ± 0.0048 mM). Additionally, in silico studies for all oxime compounds were performed to investigate the binding interactions with the active site of the urease enzyme compared to thiourea. Furthermore, the drug-likeness of the synthesized oxime compounds was also predicted.


2021 ◽  
Author(s):  
Muhammad Saleem ◽  
Ayesha Perveen ◽  
Erum Akbar Hussain ◽  
Abdul Rehman ◽  
Majid Khan ◽  
...  

Abstract Five new 2,4,6-triarylpyridine analogues with potential biological importance have been synthesized using the multicomponent reaction (MCR) solid support catalyst synthetic approach. This green synthesis furnished method simplicity, reduce reaction time, and excellent yield, along with an additional feature of catalyst reusability. A number of spectroscopic techniques such as 1H-NMR, IR, and mass spectrometry, confirmed structures of the newly synthesized compounds. Antibacterial and anti-urease activities of these compounds were evaluated. Results revealed that compounds 4a, 4c, 4d, and 4e exhibit significant inhibition against gram-positive bacterial pathogens. Furthermore, all synthesized compounds showed potent urease inhibitory activity with IC50 values ranging from 12.8 ± 1.04 to 23.7 ± 0.23 µM when compared with the standard inhibitor thiourea (IC50 21.0 ± 0.23 µM).In addition, the synthesized derivatives were subjected to density functional theory (DFT) calculations (DFT) to determine the energy of the molecules having biological potential.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Asad Hamad ◽  
Mohsin Abbas Khan ◽  
Irshad Ahmad ◽  
Ruqaiya Khalil ◽  
Muhammad Khalid ◽  
...  

AbstractCurrent research is based on biology-oriented synthesis of sulphadiazine derivatives and determination of their urease inhibitory activity. In this regard, a series of (E)-4-(benzylideneamino)-N-(pyrimidin-2-yl)benzenesulfonamide was synthesized from sulphadiazine and substituted aromatic aldehydes. The structures of synthesized compounds were ascertained by spectroscopic techniques, such as, FTIR, NMR and HRMS analysis, and in-vitro and in-silico investigation were carried out for the inhibition of urease. Ureases are harmful for humans by producing by-products of urea (ammonia and carbon dioxide). The most active compound (3l) against urease exhibited IC50 value of 2.21 ± 0.45 µM which is 10 times more potent than the standard thiourea (20.03 ± 2.06 µM). It is noteworthy that most of our synthesized compounds showed significant to excellent activities against urease enzyme and most of them substituted by halogen or hydroxy groups at ortho and para positions in their structures. Inhibition of enzyme by the synthesized analogues was in descending order as 3l > 3a > 3b > 3q > 3e > 3o > 3s > 3t > 3g > 3k > 3r > 3f > 3m > 3p > 3n > 3j > 3i > 3h. Moreover, molecular docking studies were performed to rationalize the binding interactions of the synthesized motifs with the active pocket of the urease enzyme. The synthesized sulphadiazine derivatives (3a–u) were found to be non-toxic, and presented passive gastrointestinal absorption.


2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110445
Author(s):  
Tamfu Alfred Ngenge ◽  
Selcuk Kucukaydin ◽  
Ozgur Ceylan ◽  
Mehmet Emin Duru

In this study, Melaleuca alternifolia (Maiden and Betche) Cheel (tea tree) oil and C. sinensis (L.) Osbeck (orange) oil was procured, and their chemical compositions were characterized by gas chromatography coupled with mass spectrometry, with co-injection using authentic samples. The oils were rich in monoterpene hydrocarbons making up 84.5% of C. sinensis and 48.9% of M. alternifolia oils. High amounts of oxygenated monoterpenoids were also identified in C. sinensis (9.6%) and M. alternifolia (49.3%) oils. The three most abundant compounds were limonene (71.2%), linalool (5.5%), and β-myrcene (5.1%) in C. sinensis, and terpinen-4-ol (45.6%), γ-terpinene (19.4%) and α-terpinene (9.3%) in M. alternifolia. Enzyme inhibitions (anticholinesterase, antiurease, antityrosinase) of both essential oils were evaluated. In acetylcholinesterase assay, M. alternifolia and C. sinensis had inhibition concentration (IC50) values of 153.7 ± 1.25 and 96.4 ± 1.0 µg/mL, respectively as compared to 5.42 ± 0.11 µg/mL for galantamine, while in butyrylcholinesterase assay, M. alternifolia (IC50 = 85.6 ± 0.7 µg/mL) and C. sinensis (IC50 = 127.8 ± 0.6 µg/mL) exhibited moderate activities compared to galantamine (IC50 = 45.8 ± 0.8 µg/mL). In the urease inhibitory activity, essential oils of C. sinensis and M. alternifolia showed 48.4% ± 0.9% and 30.6% ± 0.7% inhibitions at 200 µg/mL concentration, respectively. Quorum sensing (QS) mediated violacein production in Chromobacterium violaceum CV12472 was inhibited by 100% at minimum inhibitory concentration (MIC) values for both oils while showing QS inhibition diameter zones in C. violaceum of 22.5 ± 0.4 mm and 14.3 ± 0.5 mm for C. sinensis and M. alternifolia oils, respectively at MIC concentration. The good quorum-sensing potential indicates that these oils can suppress microbial resistance and severity of infections.


2021 ◽  
pp. 1-6
Author(s):  
Ejike Onwudiegwu Okpala ◽  
Patricia Akpomedaye Onocha ◽  
Muhammad Shaiq Ali ◽  
Sadia Zikr- Ur-Rehmen ◽  
Mehreen Lateef
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