Biomedical subjects
Publications and source records attributed to L Fontanella.
As a part of a research on analgesic compounds 0-(4-methoxyphenyl)carbamoyl-3-aminopropiophenone oximes, 0-(4-methoxyphenyl)-carbamoyl-3-aminomethylcamphor oximes and 4-(4-methoxyphenyl)semicarbazones of 3-aminopropiophenones were prepared. The analgesic activity of these compounds was tested and the results of pharmacological screening are discussed.
The synthesis of the above-mentioned compounds, starting from the diethyl ester of 2,5-pyrrolidine dicarboxylic acid, is reported. The cis and trans isomers od the 2-phenylsubstituted acid were separated, and the trans form was resolved into the two chiral forms. Some amides were also prepared from these acids. The thio analogs (XIII) and (XVI) and the partially reduced derivatives (XIV) were synthesized. Some amides (VI) showed an interesting anti-anxiety effect in pharmacological models.
Compounds with potential activity on the Central Nervous System were prepared starting either from 2,5-diethoxycarbonylpyrrolidine or from N-benzyloxycarbonyl-2,5-pyrrolidinedicarboxylic acid anhydride. By the Arndt-Eistert reaction it was possible to obtain chain lengthening at position 6. The carboxy group was also successfully reduced to a hydroxymethyl group. The synthetic work was completed with the synthesis of some derivatives having a phenyl ring condensed at position 7 and 8. Some pharmacological data on the Central Nervous System depressant activity of the prepared compounds are also reported.
The AA. describe the synthesis of some methyl esters of 2-alkyl or 2-aryl-2,3,5, 9b -tetrahydro-1,3-dioxo-1H-imidazo[5,1-a] isoindol -5-carboxylic acids and of the corresponding acids. From these acids some aliphatic and heterocyclic amides were synthesized. The pharmacological data of these compounds are also reported.
The report describes the synthesis and pharmacology of some new derivatives of 1-(m or p-chlorophenyl)-2-imidazolidinone. These compounds were obtained either by reacting an amine with an N-(2-chloroethyl)-2-imidazolidinone or by reacting a 2-chloroethylamine with an N-substituted-2-imidazolidinone. Two compounds (II f, h) showed interesting psychotropic activity.
The Authors describe the synthesis of some quaternary salts of the hexahydro-1H-2,6-methanopyrrolo[1,2-a]pyrazines mono or disubstituted at carbon-4. These were obtained directly by cyclization of the corresponding diazabicyclooctanes, by formation of a substituted ethylenic bridge between the two nitrogen atoms. The compounds were pharmacologically screened; the hypothesis of enhancement of curare-like activity in comparison with the unsubstituted derivatives was not confirmed.
The synthesis of two new series of 3,8-diazabicyclo [3.2.1] octane derivatives is described. The first series includes some 3-(or 8)-allyl and 3-(or 8)-(3,3-dimethylallyl) derivatives of 3,8-diazabicyclo [3.2.1] octane and 3,8-diazabicyclo [3.2.1] octane-2-one. The second series includes some esters and carbamates of 3-(3-hydroxy-3-methyl)butyl-3,8-diazabicyclo [3.2.1] octane. Two new 3,8-diazabicyclo [3.2.1] octane derivatives structurally related to propoxyphene are also described. Some pharmacological data of these compounds are reported.
As a part of research on 3,8-diazabicyclo [3,2,1] octanes, the Authors report on the synthesis of some amides of methyl, phenyl and cyclohexyltropic acid, potentially active as antiparkinson agents. Also reported is the synthesis of some compounds similar to two known drugs, Caramiphene and Cycrimine. These compounds differ from the said drugs in having a 3,8-diazabicyclo [3,2,1] octane as a basic moiety.
The Authors describe the synthesis of some 8-acyl-3-methyl-3,8-diazabicyclo[3.2.1]octanes and 3-acyl-8-methyl-3,8-diazabicylo[3.2.1] octanes. The compounds were prepared by acylation of the corresponding methyl derivatives with the purpose of obtaining antiinflammatory compounds. The synthesis of some 3-alkyl-8-propionyl-3,8-diazabicylo[3.2.1]octanes is also described. These compounds were prepared in analogy with some 8-pripionyl-3,8-diazabicyclo[3.2.1]octanes endowed with high analgesic and antiinflammatory activity.
The synthesis of 1-phenyl-1,5-dihydro-2,4-benzoxazepin-3(4H)-ones (II), of 5-phenyl-1,5-dihydro-2,4-benzoxazepin-3(4H)-ones (III) and of the 7-chloro substituted analogs is described. These compounds were prepared by reacting the corresponding amino alcohols with COCl2 in the presence of Na2CO3. The reactivity of some compounds of this series in acid or basic media is also described.
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