Fragment based screening and hit‐based substructure search: Rapid discovery of 8‐hydroxyquinoline‐7‐carboxylic acid as a low‐cytotoxic, nanomolar metallo β‐lactamase inhibitor

2021 ◽  
Author(s):  
Woo Shik Shin ◽  
Megin E. Nguyen ◽  
Alexander Bergstrom ◽  
Isabella R. Jennings ◽  
Michael W. Crowder ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Substructure Search ◽  
Lactamase Inhibitor

scholarly journals Synthesis, characterization and metal coordination of a potential β-lactamase inhibitor: 5-Methyl-2-phenoxymethyl-3- H -imidazole-4-carboxylic acid (PIMA)

2017 ◽  
Vol 10 (8) ◽  
pp. 1061-1069
Author(s):  
Chiara Romagnoli ◽  
Fabio Prati ◽  
Rois Benassi ◽  
Giulia Orteca ◽  
Monica Saladini ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Metal Coordination ◽  
Lactamase Inhibitor

scholarly journals Discovery of 1-Hydroxypyridine-2(1H )-thione-6-carboxylic Acid as a First-in-Class Low-Cytotoxic Nanomolar Metallo β-Lactamase Inhibitor

ChemMedChem ◽  
2017 ◽  
Vol 12 (11) ◽  
pp. 845-849 ◽  
Author(s):  
Woo Shik Shin ◽  
Alexander Bergstrom ◽  
Robert A. Bonomo ◽  
Michael W. Crowder ◽  
Ramaiah Muthyala ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Lactamase Inhibitor

ChemInform Abstract: Synthesis of (5R)-(Z)-6-(1-Methyl-1,2,3-triazol-4-ylmethylene)penem-3- carboxylic Acid, a Potent Broad Spectrum β-Lactamase Inhibitor, from 6-Aminopenicillanic Acid.

ChemInform ◽  
2010 ◽  
Vol 25 (18) ◽  
pp. no-no
Author(s):  
N. F. OSBORNE ◽  
R. J. ATKINS ◽  
N. J. P. BROOM ◽  
S. COULTON ◽  
J. B. HARBRIDGE ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Broad Spectrum ◽  
Lactamase Inhibitor

Fibrinolytic Activity of Cerebro-Spinal Fluid and the Development of Artificial Cerebral Haematomas in Dogs

1969 ◽  
Vol 21 (02) ◽  
pp. 294-303 ◽  
Author(s):  
H Mihara ◽  
T Fujii ◽  
S Okamoto
Keyword(s):  
Cerebrospinal Fluid ◽  
Carboxylic Acid ◽  
Fibrinolytic Activity ◽  
Clinical Implications ◽  
Trans Form ◽  
Plate Method ◽  
Blood Samples ◽  
Fibrin Plate ◽  
The Brain

SummaryBlood was injected into the brains of dogs to produce artificial haematomas, and paraffin injected to produce intracerebral paraffin masses. Cerebrospinal fluid (CSF) and peripheral blood samples were withdrawn at regular intervals and their fibrinolytic activities estimated by the fibrin plate method. Trans-form aminomethylcyclohexane-carboxylic acid (t-AMCHA) was administered to some individuals. Genera] relationships were found between changes in CSF fibrinolytic activity, area of tissue damage and survival time. t-AMCHA was clearly beneficial to those animals given a programme of administration. Tissue activator was extracted from the brain tissue after death or sacrifice for haematoma examination. The possible role of tissue activator in relation to haematoma development, and clinical implications of the results, are discussed.

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