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[Pharmacological characterization of novel pyridazines. Part 1: Physicochemical parameters, acute toxicity and action on the central nervous system (author's transl)].
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The author determined the distribution coefficients (in n-octanol/water) and the RM values (thin-layer chromatographically, using two solvent systems) of 17 newly synthetized pyridazines. These determinations evidenced that the majority of these compounds are relatively polar. Altogether the acute
Syntheses, calcium channel antagonist and anticonvulsant activities of substituted 1,4-dihydro-3,5-pyridinedicarboxylates containing various 3-alkyl ester substituents.
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A group of 3-alkyl 5-isopropyl 4-aryl-1,4-dihydro-2,6-dimethyl- 3,5-pyridinedicarboxylates 10-20 containing an amine, quaternary ammonium, aryl (heteroaryl)alkenyl, 4-(4-fluorophenyl)- piperazin-1-yl or methoxy moiety in the C-3 alkyl ester R-substituent in combination with a C-4 phenyl ring bearing
Cyclic analogs of galanin and neuropeptide Y by hydrocarbon stapling.
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Hydrocarbon stapling is an effective strategy to stabilize the helical conformation of bioactive peptides. Here we describe application of stapling to anticonvulsant neuropeptides, galanin (GAL) and neuropeptide Y (NPY), that are implicated in modulating seizures in the brain. Dicarba bridges were
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