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
Conformationally Restricted Grp94-Selective Inhibitors
Sign Up to like & getrecommendations! Published in 2025 at "ACS Omega"
DOI: 10.1021/acsomega.4c06661
Abstract: Selective inhibition of glucose regulated protein 94 (Grp94), the most structurally unique isoform of heat shock protein 90 (Hsp90), has been implicated in the treatment of various disease states, including primary open-angle glaucoma and metastatic… read more here.
Keywords: restricted grp94; conformationally restricted; selective inhibitors; grp94 selective ... See more keywords
Cobalt-catalyzed conformationally restricted alkylarylation enables divergent access to Csp3-rich N-heterocycles
Sign Up to like & getrecommendations! Published in 2024 at "Chemical Science"
DOI: 10.1039/d4sc04056b
Abstract: Due to the intrinsic spatial orientation and structural novelty, Csp3-rich N-heterocycles have been recognized as increasingly sought-after scaffolds as compared to the aromatic ring-based moieties, which have generated considerable recent attention in drug discovery. Hence,… read more here.
Keywords: conformationally restricted; rich heterocycles; catalyzed conformationally; cobalt catalyzed ... 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