107 articles for thisTarget
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Novel mechanism of inhibiting beta-lactamases by sulfonylation using beta-sultams.
The University of Huddersfield
Screening and Design of Inhibitor Scaffolds for the Antibiotic Resistance Oxacillinase-48 (OXA-48) through Surface Plasmon Resonance Screening.
Uit The Arctic University of Norway
Azolylthioacetamide: A Highly Promising Scaffold for the Development of Metallo-ß-lactamase Inhibitors.
North-West University
2-Substituted 4,5-dihydrothiazole-4-carboxylic acids are novel inhibitors of metallo-ß-lactamases.
Baylor College of Medicine
SCO-1, a novel plasmid-mediated class A beta-lactamase with carbenicillinase characteristics from Escherichia coli.
Institut Pasteur Hellenique
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
4-Substituted trinems as broad spectrum beta-lactamase inhibitors: structure-based design, synthesis, and biological activity.
Lek Pharmaceuticals
Chromosome-encoded narrow-spectrum Ambler class A beta-lactamase GIL-1 from Citrobacter gillenii.
Bicetre Hospital
Use of novel boronic acid transition state inhibitors to probe substrate affinity in SHV-type extended-spectrum beta-lactamases.
Veterans Affairs Medical Center
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
Northwestern University
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening.
Northwestern University
Structure-based design of beta-lactamase inhibitors. 2. Synthesis and evaluation of bridged sulfactams and oxamazins.
F. Hoffmann-La Roche
Design, synthesis, and evaluation of 2 beta-alkenyl penam sulfone acids as inhibitors of beta-lactamases.
F. Hoffmann-La Roche
Design and synthesis of bridged gamma-lactams as analogues of beta-lactam antibiotics.
Aventis Pharma
The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives.
University of Huddersfield
Design, synthesis and bioactivity evaluation of tribactam beta lactamase inhibitors.
Lek
The synthesis and SAR of rhodanines as novel class C beta-lactamase inhibitors.
The R. W. Johnson Pharmaceutical Research Institute
The synthesis and lactamase inhibitory activity of 6-(carboxymethylene)penicillins and 7-(carboxymethylene)cephalosporins
TBA
Side chain SAR of bicyclicß-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712.
Merck Research Labs
Thiophenyl oxime-derived phosphonates as nano-molar class C beta-lactamase inhibitors reducing MIC of imipenem against Pseudomonas aeruginosa and Acinetobacter baumannii.
Merck
Synthesis and SAR of novel benzoxaboroles as a new class of β-lactamase inhibitors.
Anacor Pharmaceuticals
Mechanistic studies of the inactivation of TEM-1 and P99 by NXL104, a novel non-beta-lactam beta-lactamase inhibitor.
Novexel
PER-6, an extended-spectrum beta-lactamase from Aeromonas allosaccharophila.
Bicetre Hospital
In vitro potentiation of carbapenems with ME1071, a novel metallo-beta-lactamase inhibitor, against metallo-beta-lactamase- producing Pseudomonas aeruginosa clinical isolates.
Toho University School of Medicine
Novel plasmid-encoded ceftazidime-hydrolyzing CTX-M-53 extended-spectrum beta-lactamase from Salmonella enterica serotypes Westhampton and Senftenberg.
Centre National De R£F£Rence Des Salmonella
Genetic variability among ampC genes from acinetobacter genomic species 3.
Complejo Hospitalario Universitario Juan Canalejo-Inibic
Substrate selectivity and a novel role in inhibitor discrimination by residue 237 in the KPC-2 beta-lactamase.
Case Western Reserve University
Naturally occurring Class A ss-lactamases from the Burkholderia cepacia complex.
H�Pital De Bic�Tre
Molecular and biochemical characterization of SHV-56, a novel inhibitor-resistant beta-lactamase from Klebsiella pneumoniae.
University of Bordeaux
Biochemical characterization of SHV-55, an extended-spectrum class A beta-lactamase from Klebsiella pneumoniae.
TBA
The Lys234Arg substitution in the enzyme SHV-72 is a determinant for resistance to clavulanic acid inhibition.
National Institute of Health Dr. Ricardo Jorge Av. Padre Cruz
In vitro properties of BAL30072, a novel siderophore sulfactam with activity against multiresistant gram-negative bacilli.
Basilea Pharmaceutica International
GES-13, a beta-lactamase variant possessing Lys-104 and Asn-170 in Pseudomonas aeruginosa.
Hellenic Pasteur Institute
4,7-Dichloro benzothien-2-yl sulfonylaminomethyl boronic acid: first boronic acid-derived beta-lactamase inhibitor with class A, C, and D activity.
Merck
Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem.
Merck Research Labs
Discovery of novel lipophilic inhibitors of OXA-10 enzyme (class D beta-lactamase) by screening amino analogs and homologs of citrate and isocitrate.
University of Louvain
Mechanistic support for the stepwise process for inactivation of class A β-lactamases by clavulanate
TBA
Biochemical Characterization of SFC-1, a class A carbapenem-hydrolyzing beta-lactamase.
University of Aveiro
TEM-158 (CMT-9), a new member of the CMT-type extended-spectrum beta-lactamases.
Chu Clermont-Ferrand
Plasmid-encoded ACC-4, an extended-spectrum cephalosporinase variant from Escherichia coli.
Institute
Interactions of ceftobiprole with beta-lactamases from molecular classes A to D.
Johnson & Johnson Pharmaceutical Research and Development
Biochemical characterization of PER-2 and genetic environment of blaPER-2.
Universidad De Buenos Aires
A high-throughput screen for aggregation-based inhibition in a large compound library.
University of California San Francisco
Recent advances in β-lactamase inhibitor chemotypes and inhibition modes.
Xihua University
Structure-activity relationship of 6-methylidene penems bearing 6,5 bicyclic heterocycles as broad-spectrum beta-lactamase inhibitors: evidence for 1,4-thiazepine intermediates with C7 R stereochemistry by computational methods.
Wyeth Research
Structure-activity relationship of 6-methylidene penems bearing tricyclic heterocycles as broad-spectrum beta-lactamase inhibitors: crystallographic structures show unexpected binding of 1,4-thiazepine intermediates.
Wyeth Research
Mechanism of inactivation of beta-lactamases by novel 6-methylidene penems elucidated using electrospray ionization mass spectrometry.
Wyeth Research
Penicillin-derived inhibitors that simultaneously target both metallo- and serine-beta-lactamases.
Southern Methodist University
Spirocyclopropyl beta-lactams as mechanism-based inhibitors of serine beta-lactamases. Synthesis by rhodium-catalyzed cyclopropanation of 6-diazopenicillanate sulfone.
Wyeth Research
Structure-based approach for binding site identification on AmpC beta-lactamase.
Northwestern University
Cephalosporin-derived inhibitors of beta-lactamase. Part 4: The C3 substituent.
Southern Methodist University
Allyl and propargyl substituted penam sulfones as versatile intermediates toward the syntheses of new beta-lactamase inhibitors.
Wyeth-Ayerst Research
Specificity of extended O-aryloxycarbonyl hydroxamates as inhibitors of a class C β-lactamase.
Wesleyan University
Synthesis and biological activities of an alpha-methyl and a beta-methyl carbapenem and the corresponding unsubstituted compound.
University of Munich
The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.
Southern Methodist University
The synthesis and evaluation of 2-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.
Southern Methodist University
Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.
Merck Research Laboratories
Synthesis and SAR of thioester and thiol inhibitors of IMP-1 metallo-beta-lactamase.
Merck Research Laboratorie
The synthesis and evaluation of 6-alkylidene-2'beta-substituted penam sulfones as beta-lactamase inhibitors.
Southern Methodist University
6-(1-Hydroxyalkyl))penam sulfone derivatives as inhibitors of class A and class C beta-lactamases II.
Wyeth-Ayerst Research
6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C beta-lactamases I.
Wyeth-Ayerst Research
Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase.
Northwestern University Medical School
Structure-based design of beta-lactamase inhibitors. 1. Synthesis and evaluation of bridged monobactams.
F. Hoffmann-La Roche
Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.
University of Oxford
BEL-2, an extended-spectrum beta-lactamase with increased activity toward expanded-spectrum cephalosporins in Pseudomonas aeruginosa.
H�Pital De Bic�Tre
Molecular and biochemical characterization of the natural chromosome-encoded class A beta-lactamase from Pseudomonas luteola.
Institut Pasteur
Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila.
University of Liege
SB-202742, a novel beta-lactamase inhibitor isolated from Spondias mombin.
Smithkline Beecham Pharmaceuticals
Synthesis and beta-lactamase inhibitory properties of 2 beta-[(1,2,3-triazol-1-yl)methyl]-2 alpha-methylpenam-3 alpha-carboxylic acid 1,1-dioxide and related triazolyl derivatives.
TBA
5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5-azaspiro[2.5]octane-8-carboxylic acid derivatives as novel JAK kinase inhibitors
Leo Pharma
Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
Ardelyx
JAK kinase inhibitor compounds for treatment of respiratory disease
Theravance Biopharma R&D Ip
6-amino-5,6,7,8-tetrahydronaphthalen-2-yl or 3-aminochroman-7-yl derivatives
Hoffmann-La Roche
Flavonoids: true or promiscuous inhibitors of enzyme? The case of deoxyxylulose phosphate reductoisomerase.
University of Strasburg
Substituted pyridinyl-pyrimidines and their use as medicaments
Boehringer Ingelheim International
Dipeptidyl peptidase-IV inhibiting compounds, methods of preparing the same, and pharmaceutical compositions containing the same as active agent
Lg Life Sciences
6-(N-benzoylamino)purine as a novel and potent inhibitor of xanthine oxidase: inhibition mechanism and molecular modeling studies.
National Institute of Pharmaceutical Education and Research
Molecular and pharmacological characterization of native cortical gamma-aminobutyric acidA receptors containing both alpha1 and alpha3 subunits.
Universidad De Sevilla
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
University of North Carolina At Chapel Hill
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.
Bristol-Myers Squibb
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.
Karo Bio
Pharmacophores incorporating numerous excluded volumes defined by X-ray crystallographic structure in three-dimensional database searching: application to the thyroid hormone receptor.
Karo Bio
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor.
Karo Bio
Pyridone derivatives as potent and selective VLA-4 integrin antagonists.
Glaxosmithkline
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Merck Research Laboratories
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.
Merck Research Laboratories