Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114359
Abstract: N-Methyl-d-aspartate (NMDA) receptors containing one or two GluN2B subunits play a crucial role in a variety of neurodegenerative diseases, such as Alzheimer's and Huntington's disease. In order to increase selectivity for GluN2B NMDA receptors, the… read more here.
Keywords: synthesis biological; biological evaluation; conformationally restricted; affinity ... See more keywords
Synthesis and photophysical properties of conformationally restricted difluoroboron β-diketonate complexes of 1-indanone derivatives
Sign Up to like & getrecommendations! Published in 2020 at "Tetrahedron"
DOI: 10.1016/j.tet.2020.131457
Abstract: Abstract A series of conformationally restricted difluoroboron β-diketonate complexes (BF2bdks) was easily synthesized from (Z)-2-(1-arylhydroxyliden)-1-indanone derivatives in good to excellent yields. These dyes displayed the lowest energy absorption maxima in the range of 370–408 nm and… read more here.
Keywords: difluoroboron; difluoroboron diketonate; conformationally restricted; diketonate complexes ... See more keywords
Conformationally Restricted σ1 Receptor Antagonists from (-)-Isopulegol.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c02081
Abstract: Antagonists at σ1 receptors have great potential for the treatment of neuropathic pain. Starting from monoterpene (-)-isopulegol (1), aminodiols 8-11 were obtained and transformed into bicyclic 13-16 and tricyclic ligands 19-22. Aminodiols 8-11 showed higher… read more here.
Keywords: affinity; antagonists isopulegol; conformationally restricted; higher affinity ... See more keywords
Discovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer's Agents by Structure-Based Design.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00751
Abstract: Alzheimer's disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consist of various factors; thus, there is a call for alternative approaches to tackle the multifaceted… read more here.
Keywords: glutaminyl cyclase; discovery conformationally; conformationally restricted; restricted human ... See more keywords
Conformationally Restricted Dipeptide-Based Nanoparticles for Delivery of siRNA in Experimental Liver Cirrhosis
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c05292
Abstract: Liver cirrhosis is a major health problem with multiple associated complications. The presently available drug delivery systems showed moderate site-specific delivery of antifibrotic molecules to the diseased liver; therefore, research on more effective and selective… read more here.
Keywords: liver cirrhosis; delivery; experimental liver; conformationally restricted ... See more keywords
Synthetic Methods for the Preparation of Conformationally Restricted Analogues of Nicotine.
Sign Up to like & getrecommendations! Published in 2021 at "Molecules"
DOI: 10.3390/molecules26247544
Abstract: In the context of naturally occurring nitrogen heterocycles, nicotine is a chiral alkaloid present in tobacco plants, which can target and stimulate nicotinic acetylcholine receptors (nAChRs), a class of ligand-gated ion channels commonly located throughout… read more here.
Keywords: conformationally restricted; restricted analogues; synthetic methods; methods preparation ... See more keywords
New Insights into Conformationally Restricted Carbonic Anhydrase Inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "Molecules"
DOI: 10.3390/molecules28020890
Abstract: This paper reports an investigation into the impact of pyridyl functional groups in conjunction with hydroxide-substituted benzenesulfonamides on the inhibition of human carbonic anhydrase (CA; EC 4.2.1.1) enzymes. These compounds were tested in vitro of… read more here.
Keywords: insights conformationally; carbonic anhydrase; anhydrase; conformationally restricted ... See more keywords
Base-Promoted Intramolecular Addition of Vinyl Cyclopropanecarboxamides to Access Conformationally Restricted Aza[3.1.0]bicycles
Sign Up to like & getrecommendations! Published in 2023 at "Molecules"
DOI: 10.3390/molecules28093691
Abstract: 3-Azabicyclo[3.1.0]hexanes are common structural components in natural products and bioactive compounds. Traditionally, the metal-mediated cyclopropanation domino reaction of chain enzymes is the most commonly used strategy for the construction of this type of aza[3.1.0]bicycle derivative.… read more here.
Keywords: base promoted; aza bicycles; conformationally restricted; promoted intramolecular ... See more keywords