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Microwave-assisted extraction of coumarin and related compounds from Melilotus officinalis (L.) Pallas as an alternative to Soxhlet and ultrasound-assisted extraction.
TLDR
On the basis of the ratio extraction yield/extraction time, MAE is proposed as the most efficient method to determine the content of coumarin, o-coumaric and melilotic acids in flowering tops of Melilotus officinalis. Expand
Identification of a potent and selective σ₁ receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.
Herein we report the synthesis, drug-likeness evaluation, and in vitro studies of new sigma (σ) ligands based on arylalkenylaminic scaffold. For the most active olefin the correspondingExpand
Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.
TLDR
Rational chemical modifications of the hit allowed the disclosure of the first reported highly selective S1P(4) antagonists with low nanomolar activity and adequate physicochemical properties suitable for further lead-optimization studies. Expand
Modulators of the Sphingosine 1-phosphate receptor 1.
TLDR
This review provides the latest advances on next-generation S1P1-R modulators from 2012 up to date, with an overview of the chemical structures, structure-activity relationships, and relevant biological and clinical properties. Expand
Sphingosine 1-phosphate receptor 1 agonists: a patent review (2013-2015)
TLDR
Clinical and preclinical studies of second generation S1P1-R agonists have been generating interesting results and may finally provide pharmacological agents with improved therapeutic profile than FTY720, particularly in terms of cardiovascular and pulmonary liabilities. Expand
Antagonists of the Kappa Opioid Receptor
Article history: Received 28 January 2014 Revised 11 March 2014 Accepted 15 March 2014 Available online 24 March 2014
Sphingosine 1-phosphate receptor agonists: a patent review (2010 – 2012)
TLDR
This review provides the patent literature from 2010 to date on S1P-R agonist molecules and their relevant biological properties and reveals a discrete number of reviewed molecules with a promising clinical outlook in transplantation, inflammation, cancer and autoimmune settings. Expand
Antagonists of the kappa opioid receptor.
The research community has increasingly focused on the development of OPRK antagonists as pharmacotherapies for the treatment of depression, anxiety, addictive disorders and other psychiatricExpand
Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).
In order to investigate the molecular features involved in sigma receptors (sigma-Rs) binding, new compounds based on arylalkylaminoalcoholic, arylalkenyl- and arylalkylaminic scaffolds wereExpand
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