Synthesis and Biological Activity of Spiro [isocoumarin-piperidines] and Reltaed Compounds. I

doi:10.1248/CPB.29.402

Paper

Synthesis and Biological Activity of Spiro [isocoumarin-piperidines] and Reltaed Compounds. I

Published Feb 25, 1981 · M. Yamato, K. Hashigaki, M. Ikeda

Chemical & Pharmaceutical Bulletin

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Abstract

1'-Alkylspiro [isochroman-3, 4'-piperidin]-1-ones (2) and 1'-alkylspiro [isochroman-4, 4'-piperidines] (4 and 5) were prepared and examined for analgesic activity. Several of the 4-spiro compounds (3, 4, and 5) were found to have analgesic activity as potent as that of aminopyrine, while the 3-spiro compounds (2) were inactive. Further pharmacological studies revealed that several of these compounds inhibited the histamine release induced by compound 48/80 from isolated rat peritoneal mast cells.

In Vitro Study

Study Snapshot

Spiro [isochroman-4, 4'-piperidines] show analgesic activity as potent as aminopyrine, while 3-spiro compounds are inactive and inhibit histamine release from mast cells.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and Biological Activity of Spiro [isocoumarin-piperidines] and Reltaed Compounds. I

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References

A method for the fluorometric assay of histamine in tissues.

This fluorometric method accurately estimates histamine levels in tissues, with concentrations as low as 0.005 g/ml, and can detect low levels in brain tissue.

Citations

Research progress in biological activities of isochroman derivatives.

Isochroman derivatives show diverse biological activities and potential therapeutic applications, including central nervous system, antioxidant, antimicrobial, antihypertensive, antitumor, and anti-inflammatory agents.

Conformational dimorphism of isochroman-1-ones in the solid state

Isochroman-1-one derivatives can adopt two distinct conformations in the solid state, with the open conformer being thermochemically more stable.

Lateral Lithiation Reactions Promoted by Heteroatomic Substituents

Heteroatom-facilitated lateral lithiation reactions play a crucial role in the synthesis of carbocyclic aromatic and heteroaromatic systems, with applications in functionalization, chain extensions, and fused systems.

Chirale 2-Benzopyran-3-carbonsäure-Derivate durch Oxa-Pictet-Spengler-Reaktion von (S)-3-Phenylmilchsäure-Derivaten

The oxa-Pictet-Spengler reaction of (S)-3-phenyllactic acid derivatives yields chiral 2-benzopyran-3-carboxylates with enantiomeric purity greater than 96% ee.

Synthesis of spiro[piperidine-4,Cn'-hetero(carbo)cycles]

Spiro[piperidine-4,Cn'-hetero(carbo)cycles] show potential as biologically active compounds due to their spiro-condensed piperidine rings and diverse carbocycle and heterocycle structures.