Indolizines II: search for potential oral hypoglycemic agents.

doi:10.1002/JPS.2600640211

Paper

Indolizines II: search for potential oral hypoglycemic agents.

Published Feb 1, 1975 · A. De, B. Saha

Journal of pharmaceutical sciences

Q2 SJR score

27

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0

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Abstract

A few 1,2-bis(N-alkylaminomethyl)indolizines, simple indolizinecarboxylic acids, and several 6-alkoxyindolizine-2-carboxylic acids were synthesized and screened as possible oral hypoglycemic agents. The absence of any significant hypoglycemic activity excludes these compounds from the predicted structural lead provided by some hypoglycemic Vinca alkaloids, such as vincamine, vindoline, and vindolinine, having the indolizine ring as one structural component. But an extension of the rationale that indolizines are also the structural components of some carcinolytic Vinca alkaloids, such as vincristine and vinblastine, used in cancer chemotherapy provided encouraging results. One indolizine derivative showed significant antineoplastic activity in Ehrlich ascites carcinoma.

In Vitro Study

Study Snapshot

Indolizines show no significant hypoglycemic activity, but may have potential in cancer chemotherapy due to their structural components in carcinolytic Vinca alkaloids.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Paper

Indolizines II: search for potential oral hypoglycemic agents.

References

Search for potential oral hypoglycemic agents: synthesis and activity of 2-(N-alkylaminomethyl)indolizines.

2-(N-alkylaminomethyl)indolizines show weak oral hypoglycemic activity, but some show anti-Parkinson and marginal anti-inflammatory properties.

The effect of 5-methylpyrazole-3-carboxylic acid on carbohydrate and free fatty acid metabolism.

U-19425 is a potent hypoglycemic agent with a primary action on fat metabolism, and its effect on glucose oxidation and blood sugar depression may be secondary to initial plasma FFA depression.

A PHOTOMETRIC ADAPTATION OF THE SOMOGYI METHOD FOR THE DETERMINATION OF GLUCOSE

The new arsenomolybdate reagent combined with Somogyi's micro reagent provides stable and reproducible color for glucose determination in biological material, improving reproducibility and stability.

Citations

Novel Tandem Three Consecutive Reactions: Aza-Wittig, Imine Condensation and Electrophilic Aromatic Substitution Strategy to Indolizine Synthesis

This study demonstrates a novel tandem three-consecutive reaction strategy for indolizine synthesis using ethyl (Z)-3-(heteroaryl/aryl)-2-((triphenyl-5-phosphaneylidene) amino) acrylates

Cytotoxic constituents from the wheat plant pathogen Parastagonospora nodorum SN15

The wheat plant pathogen Parastagonospora nodorum SN15 produces cytotoxic compounds with potential for future drug discovery, showing specific features towards cancer cells compared to normal fibroblasts.

Brønsted-acid-catalyzed selective Friedel-Crafts monoalkylation of isatins with indolizines in water.

This study demonstrates a mild, surfactant-accelerated method for selectively synthesizing 3-Hydroxy-3-indolizinyl-2-oxindole scaffolds in water using diphenylphosphate catalyst and 3-Hydroxy-3-indolizinyl-2-

Combining Indolizines and Isatins via Brønsted-Acid Catalyzed Friedel-Crafts Alkylation in Water

This study demonstrates a novel method for synthesizing new 3-hydroxy-3-indolizinyl-2-oxindoles scaffolds in water using diphenylphosphate as catalyst and sodium dodecyl sulfate as surfactant, with up to 99% yield.

An Eco-Friendly Stereoselective Synthesis of Novel Derivatives of Indeno[1,2-b]Pyrrole and Indeno[1,2-c]Pyridazine

This eco-friendly method efficiently synthesizes pharmaceutically interesting indenopirrole derivatives, offering environmental friendliness, mild reaction conditions, and simple work-up without chromatographic purification.