Development of Urease Inhibitors by Fragment‐Based Dynamic Combinatorial Chemistry
Sign Up to like & getrecommendations! Published in 2022 at "ChemMedChem"
DOI: 10.1002/cmdc.202200307
Abstract: In this study, fragment‐based dynamic combinatorial chemistry (DCC) was explored for the development of novel urease inhibitors. Based on a rationally designed fragment, two iteratively evolved dynamic combinatorial libraries (DCLs) were generated and screened in… read more here.
Keywords: fragment based; dynamic combinatorial; combinatorial chemistry; chemistry ... See more keywords
Hydrazine clubbed 1,3-thiazoles as potent urease inhibitors: design, synthesis and molecular docking studies
Sign Up to like & getrecommendations! Published in 2020 at "Molecular Diversity"
DOI: 10.1007/s11030-020-10057-7
Abstract: Abstract Synthesis of a novel series of hydrazine clubbed 1,3-thiazoles ( 5a–m ) has been described by reacting hydrazine-1-carbothioamides ( 3a–k ) with α -chloro- or bromo-acetophenones ( 4a–d ) in refluxing ethanol in good… read more here.
Keywords: urease inhibitors; clubbed thiazoles; potent urease; hydrazine clubbed ... See more keywords
Design, synthesis, in vitro Evaluation and docking studies on dihydropyrimidine-based urease inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2017.07.003
Abstract: In our previous report, we have identified 3,4-dihydropyrimidine scaffold as promising class of urease inhibitor in a structure based virtual screen (SBVS) experiment. In present study, we attempted to optimize the scaffold by varying C-5… read more here.
Keywords: design synthesis; evaluation docking; urease inhibitors; docking studies ... See more keywords
Molecular inclusion process of urease inhibitors into cyclodextrins: A theoretical study
Sign Up to like & getrecommendations! Published in 2017 at "Chemical Physics Letters"
DOI: 10.1016/j.cplett.2017.03.010
Abstract: Abstract This paper reports a theoretical investigation on formation of host/guest inclusion complexes of two urease inhibitors into cyclodextrins. The main goals were to modeling and propose new supramolecular delivery systems of urease inhibitors. Structures… read more here.
Keywords: inclusion; urease inhibitors; inclusion process; study ... See more keywords
Arylamino containing hydroxamic acids as potent urease inhibitors for the treatment of Helicobacter pylori infection.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.06.065
Abstract: A novel series of aniline-containing hydroxamic acids were designed, synthesized and evaluated as anti-virulence agents for the treatment of gastritis and gastric ulcer caused by Helicobacter pylori. In vitro enzyme-based screen together with in vivo assays and… read more here.
Keywords: containing hydroxamic; urease inhibitors; treatment; potent urease ... See more keywords
A cheap, simple high throughput method for screening native Helicobacter pylori urease inhibitors using a recombinant Escherichia coli, its validation and demonstration of Pistacia atlantica methanolic extract effectivity and specificity.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of microbiological methods"
DOI: 10.1016/j.mimet.2016.11.022
Abstract: Helicobacter pylori is the most frequent and persistent bacterial infection worldwide, and a risk factor for active gastritis, peptic ulcers, mucosa-associated lymphoid tissue lymphoma, and gastric cancer. Although combined antibiotics treatment is effective cases of… read more here.
Keywords: methanolic extract; recombinant escherichia; urease inhibitors; escherichia coli ... See more keywords
Bioassay-guided isolation of urease inhibitors from Ferula narthex Bioss
Sign Up to like & getrecommendations! Published in 2019 at "South African Journal of Botany"
DOI: 10.1016/j.sajb.2018.07.011
Abstract: Abstract The current study was designed to evaluate the urease inhibitory activities of the fractions of Ferula narthex Bioss, followed by bioassay guided isolation of new urease sesquiterpene coumarins, as potential urease inhibitors. The chloroform… read more here.
Keywords: urease inhibitors; ferula narthex; bioassay guided; narthex bioss ... See more keywords
Identification of novel bacterial urease inhibitors through molecular shape and structure based virtual screening approaches
Sign Up to like & getrecommendations! Published in 2020 at "RSC Advances"
DOI: 10.1039/d0ra02363a
Abstract: The enzyme urease is an essential colonizing factor of the notorious carcinogenic pathogen Helicobacter pylori (H. pylori), conferring acid resistance to the bacterium. Recently, antibiotic resistant strains have emerged globally with little to no alternative… read more here.
Keywords: novel bacterial; shape; urease inhibitors; screening ... See more keywords
Research Status and Progress of Inhibitory Effects and Inhibitory Mechanism of Complex-Type Urease Inhibitors - A Review
Sign Up to like & getrecommendations! Published in 2019 at "Communications in Soil Science and Plant Analysis"
DOI: 10.1080/00103624.2019.1579826
Abstract: ABSTRACT The widespread presence of urease in agricultural settings places enormous pressure on the soil environment. Urease inhibitors have been used as promising biochemical methods in reducing urease efficiency to ensure food security and agricultural… read more here.
Keywords: research; urease inhibitors; type urease; complex type ... See more keywords
Identification of novel urease inhibitors: pharmacophore modeling, virtual screening and molecular docking studies
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2018.1546620
Abstract: Abstract Pharmacophore modeling and atom-based three-dimensional quantitative structure–activity relationship (3D-QSAR) have been developed on N-acylglycino- and hippurohydroxamic acid derivatives, which are known potential inhibitors of urease. This is followed by virtual screening and ADMET (absorption,… read more here.
Keywords: virtual screening; pharmacophore model; urease inhibitors; pharmacophore modeling ... See more keywords
N-monoarylacetothioureas as potent urease inhibitors: synthesis, SAR, and biological evaluation
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2019.1706503
Abstract: Abstract A urease inhibitor with good in vivo profile is considered as an alternative agent for treating infections caused by urease-producing bacteria such as Helicobacter pylori. Here, we report a series of N-monosubstituted thioureas, which… read more here.
Keywords: inhibitors synthesis; synthesis sar; sar biological; urease inhibitors ... See more keywords