A focused fragment library targeting the antibiotic resistance enzyme - Oxacillinase-48: Synthesis, structural evaluation and inhibitor design

European Journal of Medicinal Chemistry

Volumn 145, Issue , 2018, Pages 634-648

  Akhter, Sundus ^a   Lund, Bjarte Aarmo ^a   Ismael, Aya ^a   Langer, Manuel ^a   Isaksson, Johan ^a   Christopeit, Tony ^a   Leiros, Hanna Kirsti S ^a   Bayer, Annette ^a  

^a UNIVERSITY OF TROMSØ   (Norway)

Author keywords

Benzoic acid derivatives; Crystal structure; Fragments; Inhibition properties; Serine lactamase inhibitors; Structure guided drug design

Indexed keywords

3 (3' ACETAMIDOPHENYL) 5 PYRIDIN 4 YLBENZOIC ACID; 3 (3' ACETAMIDOPHENYL) 5 QUINOLIN 6 YLBENZOIC ACID; 3 BROMO 5 (QUINOLIN 6 YL)BENZOIC ACID; 3,5 DI(3 ACETAMIDOPHENYL)BENZOIC ACID; 3,5 DI(4 ACETAMIDOPHENYL)BENZOIC ACID; 3,5 DIQUINOLIN 6 YLBENZOIC ACID; ANTIBIOTIC AGENT; BENZOIC ACID DERIVATIVE; ENZYME INHIBITOR; OXACILLINASE 48; UNCLASSIFIED DRUG; BETA LACTAMASE; BETA LACTAMASE INHIBITOR; OXACILLINASE;

ANTIBIOTIC RESISTANCE; ARTICLE; CARBON NUCLEAR MAGNETIC RESONANCE; CONTROLLED STUDY; CROSS COUPLING REACTION; CRYSTALLIZATION; DRUG CONFORMATION; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; ENZYME BINDING; ENZYME CONFORMATION; ENZYME INHIBITION; IC50; SURFACE PLASMON RESONANCE; SUZUKI REACTION; X RAY CRYSTALLOGRAPHY; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; ENZYMOLOGY; ESCHERICHIA COLI; KLEBSIELLA PNEUMONIAE; METABOLISM; MOLECULAR LIBRARY; PHARMACOLOGY; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

BETA-LACTAMASE INHIBITORS; BETA-LACTAMASES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG RESISTANCE, MICROBIAL; ESCHERICHIA COLI; KLEBSIELLA PNEUMONIAE; MOLECULAR STRUCTURE; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85040582053     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2017.12.085     Document Type: Article

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