Enolate alkylation of bicyclo(2.2.2)oct-5-en-2-one and radical cyclisation - a potential approach for the construction of tricyclic carbocycles

1988 ◽  
Vol 29 (45) ◽  
pp. 5789-5792 ◽  
Author(s):  
Thennati Rajamannar ◽  
Kalpattu Kuppuswamy Balasubramanian
Keyword(s):  
Potential Approach ◽  
Enolate Alkylation

An Anthrone-Based Kv7.2/7.3 Channel Blocker with Improved Properties for the Investigation of Psychiatric and Neurodegenerative Disorders

2019 ◽  
Author(s):  
Jacob Porter ◽  
Oscar Vivas-Rodriguez ◽  
C. David Weaver ◽  
Eamonn Dickson ◽  
Abdulmohsen Alsafran ◽  
...  
Keyword(s):  
Patch Clamp ◽  
Neurodegenerative Disorders ◽  
Channel Blocker ◽  
Optimal Combination ◽  
Channel Blockers ◽  
Enolate Alkylation ◽  
Cyp Inhibition ◽  
Alkylation Reactions ◽  
Metabolic Instability

A set of novel Kv7.2/7.3 (KCNQ2/3) channel blockers was synthesized to address several liabilities of the known compounds XE991 (metabolic instability and CYP inhibition) and the clinical compound DMP 543 (acid instability, insolubility, and lipophilicity). Using the anthrone scaffold of the prior channel blockers, alternative heteroarylmethyl substituents were installed via enolate alkylation reactions. Incorporation of a pyridazine and a fluorinated pyridine gave an analog (JDP-107) with an optimal combination of potency (IC<sub>50</sub>= 0.16 𝜇M in a Kv7.2 thallium flux assay), efficacy in a Kv7.2/7.3 patch clamp assay, and drug-like properties.

Multitarget Opioid/Non-opioid Ligands: A Potential Approach in Pain Management

2016 ◽  
Vol 23 (40) ◽  
pp. 4506-4528 ◽  
Author(s):  
Rita Turnaturi ◽  
Giuseppina Arico ◽  
Giuseppe Ronsisvalle ◽  
Lorella Pasquinucci ◽  
Carmela Parenti
Keyword(s):  
Pain Management ◽  
Potential Approach ◽  
Opioid Ligands

Biofertilizers: a potential approach for sustainable agriculture development

2016 ◽  
Vol 24 (4) ◽  
pp. 3315-3335 ◽  
Author(s):  
Trishna Mahanty ◽  
Surajit Bhattacharjee ◽  
Madhurankhi Goswami ◽  
Purnita Bhattacharyya ◽  
Bannhi Das ◽  
...  
Keyword(s):  
Sustainable Agriculture ◽  
Potential Approach ◽  
Agriculture Development

scholarly journals Relativistic B-Spline R-Matrix Calculations for Electron Collisions with Ytterbium

Atoms ◽  
2021 ◽  
Vol 9 (3) ◽  
pp. 47
Author(s):  
Kathryn R. Hamilton ◽  
Klaus Bartschat ◽  
Oleg Zatsarinny
Keyword(s):  
Experimental Data ◽  
Electron Scattering ◽  
Cross Sections ◽  
Matrix Method ◽  
Model Potential ◽  
Electron Collisions ◽  
R Matrix ◽  
B Spline ◽  
Potential Approach

We have applied the full-relativistic Dirac B-Spline R-matrix method to obtain cross sections for electron scattering from ytterbium atoms. The results are compared with those obtained from a semi-relativistic (Breit-Pauli) model-potential approach and the few available experimental data.

FTIR combined with chemometric tools — a potential approach for early screening of grazers in microalgal cultures

2021 ◽  
Author(s):  
Pranali Deore ◽  
John Beardall ◽  
Yussi M Palacios ◽  
Santosh Noronha ◽  
Philip Heraud
Keyword(s):  
Early Screening ◽  
Potential Approach ◽  
Chemometric Tools

scholarly journals Controlling Product Selectivity with Nanoparticle Composition in Tandem Chemo-Biocatalytic Styrene Oxidation

2021 ◽  
Author(s):  
Derik Wilbers ◽  
Joseph Brehm ◽  
Richard Lewis ◽  
Jacqueline Van Marwijk ◽  
Thomas Davies ◽  
...  
Keyword(s):  
Heterogeneous Catalysis ◽  
Product Selectivity ◽  
Styrene Oxidation ◽  
One Pot ◽  
Potential Approach ◽  
Reaction Cascades

The combination of heterogeneous catalysis and biocatalysis into one-pot reaction cascades is a potential approach to integrate enzymatic transformations into existing chemical infrastructure. Peroxygenases, which can achieve clean C-H activation,...

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