850142-79-9Relevant academic research and scientific papers
Nucleophilic C-H Etherification of Heteroarenes Enabled by Base-Catalyzed Halogen Transfer
Puleo, Thomas R.,Klaus, Danielle R.,Bandar, Jeffrey S.
supporting information, p. 12480 - 12486 (2021/08/24)
We report a general protocol for the direct C-H etherification of N-heteroarenes. Potassium tert-butoxide catalyzes halogen transfer from 2-halothiophenes to N-heteroarenes to form N-heteroaryl halide intermediates that undergo tandem base-promoted alcohol substitution. Thus, the simple inclusion of inexpensive 2-halothiophenes enables regioselective oxidative coupling of alcohols with 1,3-azoles, pyridines, diazines, and polyazines under basic reaction conditions.
ALKYNE COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS
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Page/Page column 110, (2016/05/02)
Provided are compounds of formula (Ia) and pharmaceutically acceptable salts thereof, wherein A, B, R 1, R 2, m and n are as defined herein, which are active as inhibitors of S-Nitrosoglutathione reductase (GSNOR). These compounds prevent, inhibit, or suppress the action of GSNOR and are therefore useful in the treatment of GSNOR mediated diseases, disorders, syndromes or conditions such as, e.g., pulmonary hypertension, acute respiratory distress syndrome (ARDS), asthma, bronchospasm, cough, pneumonia, pulmonary fibrosis, interstitial lung diseases, cystic fibrosis and chronic obstructive pulmonary disease (COPD).
Boronic species as promising inhibitors of the Staphylococcus aureus NorA efflux pump: Study of 6-substituted pyridine-3-boronic acid derivatives
Fontaine, Fanny,Héquet, Arnaud,Voisin-Chiret, Anne-Sophie,Bouillon, Alexandre,Lesnard, Aurélien,Cresteil, Thierry,Jolivalt, Claude,Rault, Sylvain
, p. 185 - 198 (2015/04/14)
In response to the extensive use of antibiotics, bacteria have evolved numerous mechanisms of defense against antimicrobial agents. Among them, extrusion of the antimicrobial agents outside the bacterial cell through efflux pumps is a major cause of concern. At first limited to one or few structurally-related antibiotics, bacterial resistance have then progressed towards cross-resistance between different classes of antibiotics, leading to multidrug-resistant microorganisms. Emergence of these pathogens requires development of novel therapeutic strategies and inhibition of efflux pumps appears to be a promising strategy that could restore the potency of existing antibiotics. NorA is the most studied chromosomal efflux pump of Staphylococcus aureus; it is known to be implied in resistance of Methicillin-resistant S. aureus (MRSA) strains against a wide range of unrelated substrates, including hydrophilic fluoroquinolones. Starting from 6-benzyloxypyridine-3-boronic acid I that we previously identified as a potential inhibitor of the NorA efflux pump against the NorA-overexpressing S. aureus 1199B strain (SA1199B), we describe here the synthesis and biological evaluation of a series of 6-(aryl)alkoxypyridine-3-boronic acids. 6-(3-Phenylpropoxy)pyridine-3-boronic acid 3i and 6-(4-phenylbutoxy)pyridine-3-boronic acid 3j were found to potentiate ciprofloxacin activity by a 4-fold increase compared to the parent compound I. In addition, it has been shown that both compounds promote Ethidium Bromide (EtBr) accumulation in SA1199B, thus corroborating their potential mode of action as NorA inhibitors.
New Positive allosteric modulators of nicotinic acetylcholine receptor
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Paragraph 0173, (2013/03/26)
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.
1-‘2-(4-HYDROXYPHENYL)-2-HYDROXYETHYL!-PIPERIDIN-4-OL COMPOUNDS AS NMDA RECEPTOR ANTAGONISTS
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Page/Page column 76-77, (2010/02/11)
This invention provides a compound of the formula (I), wherein R1 and R2 independently represents a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring carbon or the like; said aryl groups havin
FUSED LACTAM COMPOUNDS
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Page/Page column 45, (2010/02/11)
This invention provides a compound the formula (I), wherein R1 represents an aryl group having from 6 to 10 ring carbon atoms etc.; R2 represents a hydrogen atom etc., n epresents 0, 1 or 2; said heteroaryl group is unsubstituted or
