Publications by authors named "Reinhardt Baudy"
Previous studies with perzinfotel (1), a potent, selective, competitive NMDA receptor antagonist, showed it to be efficacious in inflammatory and neuropathic pain models. To increase the low oral bioavailability of 1 (3-5%), prodrug derivatives (3a-h) were synthesized and evaluated. The oxymethylene-spaced diphenyl analogue 3a demonstrated good stability at acidic and neutral pH, as well as in simulated gastric fluid.
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- Researchers explored new compounds that combine elements affecting serotonin receptors and transporters, connecting them via an alkyl chain.
- They found that specific structures, particularly a certain benzopyran linked to an indole, showed better affinity for serotonin targets, especially with certain fluorine and cyano substitutions.
- The study identified that certain chemical features, like cyclobutyl groups and the arrangement of atoms at specific positions, were crucial for effective antagonism at the serotonin 1A receptor, but some compounds were not potent enough for further development.
Two novel N-methyl-d-aspartate (NMDA) antagonists with unique chemical structures, EAA-090 (2-[8,9-dioxo-2, 6-diazabicyclo[5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride), were compared with CGS-19755 (Selfotel) in ligand binding, electrophysiology, and neuroprotection assays.
View Article and Find Full Text PDFA pro-drug strategy to identify orally efficacious VLA-4 antagonists is described. Potential pro-drugs were evaluated for their physical chemical characteristics and in vitro properties, including solubility, stability, permeability and plasma stability. Based on this characterization, promising compounds were identified for in vivo pharmacokinetic evaluation.
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