Search Results - "Kneen, Clare O"
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Oxadiazolone bioisosteres of pregabalin and gabapentin
Published in Bioorganic & medicinal chemistry letters (2009)“…A series of oxadiazolone bioisosteres of pregabalin 1 and gabapentin 2 were prepared, and several were found to exhibit similar potency for the α 2-δ subunit…”
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Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors
Published in Journal of medicinal chemistry (01-10-1990)“…The synthesis and biochemical evaluation of novel 1,2,4-oxadiazole-based muscarinic agonists which can readily penetrate into the CNS is reported. Efficacy and…”
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Carboxylate bioisosteres of gabapentin
Published in Bioorganic & medicinal chemistry letters (01-05-2006)“…Ring expansion and acid replacement with tetrazole furnished a compound with a similar pattern of activity to gabapentin. A series of carboxylate bioisosteres…”
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Identification of Novel Ligands for the Gabapentin Binding Site on the α2δ Subunit of a Calcium Channel and Their Evaluation as Anticonvulsant Agents
Published in Journal of medicinal chemistry (21-05-1998)“…As part of a program to investigate the structure−activity relationships of Gabapentin (Neurontin), a number of alkylated analogues were synthesized and…”
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Tetrahydropyridyloxadiazoles: semi-rigid muscarinic ligands
Published in Journal of medicinal chemistry (01-03-1991)Get full text
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Carboxylate bioisosteres of gabapentin Dedicated to David W. Robertson in memory of his outstanding contributions as a mentor and drug hunter
Published in Bioorganic & medicinal chemistry letters (01-01-2006)“…A series of carboxylate bioisosteres of structures related to gabapentin 1 have been prepared. When the carboxylate was replaced by a tetrazole, this group was…”
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Tetrahydropyridyloxadiazoles : semirigid muscarinic ligands
Published in Journal of medicinal chemistry (01-03-1991)“…Recent studies have described novel azabicycle-based muscarinic agonists which readily penetrate into the central nervous system and are capable of displaying…”
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Investigation into the preferred conformation of gabapentin for interaction with its binding site on the α2δ subunit of a calcium channel
Published in Bioorganic & medicinal chemistry letters (07-10-1997)“…A series of conformationally restricted Gabapentin analogues has been synthesised and used to propose the preferred conformation of Gabapentin for it to bind…”
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Purification of the 5-hydroxytryptamine 5-HT3 receptor from NCB20 cells
Published in The Journal of biological chemistry (15-08-1990)“…A 5-hydroxytryptamine 5-HT3 receptor binding site has been purified from deoxycholate-solubilized NCB20 cell membranes. Purification (1,700-fold) was achieved…”
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Inotropic 'A' ring substituted sulmazole and isomazole analogs
Published in Journal of medicinal chemistry (01-08-1990)“…A series of "A" ring substituted sulmazole and isomazole analogues have been prepared and evaluated as inotropic agents. pKA's, protonation sites, and log P…”
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Inotropic activities of imidazopyridines
Published in Archiv der Pharmazie (Weinheim) (1990)“…A series of 2-substituted 1H-imidazo[4,5-b]pyridines and the isomeric 1H-imidazo[4,5-c]pyridine derivatives has been prepared and evaluated as inotropic…”
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