2-Substituted Phenethyl-3-[(N, N-dialkyl, or N-cycloalkyl)aminocarbonylethyl]-amino-6-methylpyridineの合成とスクリーニング
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Condensation of 2,6-dimethyl-3-nitropyridine (I) and substituted benzaldehydes in acetic anhydride affords 2-substituted styryl-6-methyl-3-nitro-pyridines (II). Conversion of II to 2-substituted phenethyl-3-amino-6-methylpyridines (IV) was carried out in the presence of Raney-nickel of palladiumcarbon catalyst and hydrogen. 2-Substituted phenethyl-3-[(N, N-dialkyl- or N-cycloalkyl) aminocarbonylethyl] amino-6-methylpyridines (V) were prepared by the condensation of IV with N, N-dialkyl- or N-cycloaklyl-acrylamides in the presence of a catalyst such as acetic acid in nitrogen gas. Pharmacological screenings, such as the effect of the spasmus induced by serotonin, antibarium, antiacetylcolinegic, antihistamine, analgesic, prolonged effect on sodium barbiturate sleeping time, anticonvulsant, antipyretic, depressive action on spontaneous motility, locomotion test, and antihypertensive activity, were employed, whose results are shown in Table VIII. The structure-activity relationship was not clear, but compounds No. 23,23-1,and No. 25 and 26 of V were found to have an effect on spasmus induced by serotonin and prolonged effect on sodium barbiturate sleeping time, respectively.
- 公益社団法人日本薬学会の論文
- 1971-08-25
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