Benzylpiperazine derivatives. V. Quantitative structure-activity relationships of 1-benzyl-4-diphenylmethylpiperazine derivatives for cerebral vasodilating activity.

doi:10.1248/CPB.35.4117

Paper

Benzylpiperazine derivatives. V. Quantitative structure-activity relationships of 1-benzyl-4-diphenylmethylpiperazine derivatives for cerebral vasodilating activity.

Published Oct 25, 1987 · H. Ohtaka, G. Tsukamoto

Chemical & pharmaceutical bulletin

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Abstract

The quantitative structure-activity relationships of 1-benzyl-4-diphenylmethylpiperazines for cerebral vasodilating activity and duration of action were examined. The analyses indicate that increase of the electron density on the benzylic nitrogen atom and the introduction of sterically small substituents at the para position of the diphenylmethyl moiety bring about strong interactions of the molecule with the active site and result in high potency as well as prolonged action.

In Vitro Study

Study Snapshot

Increasing electron density on the benzylic nitrogen atom and introducing small substituents at the para position of the diphenylmethyl moiety result in high potency and prolonged action of 1-benzyl-4-diphenylmethylpiperazines for cerebral vasodilation.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Benzylpiperazine derivatives. V. Quantitative structure-activity relationships of 1-benzyl-4-diphenylmethylpiperazine derivatives for cerebral vasodilating activity.

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References

Citations

Stereoselective Synthesis of (Z)-1-Benzhydryl-4-cinnamylpiperazines via the Wittig Reaction

The Wittig reaction effectively produces (E)- and (Z)-isomers of 1-benzhydryl-4-cinnamylpiperazines in a 15:85 ratio from benzhydrylpiperazine, with good yields.

History of Quantitative Structure–Activity Relationships

The QSAR paradigm has evolved over the past 50 years, with molecular descriptors playing a crucial role in high-throughput screening and database development.

Ligustrazine derivatives. Part 3: Design, synthesis and evaluation of novel acylpiperazinyl derivatives as potential cerebrocardiac vascular agents.

Novel acylpiperazinyl Ligustrazine derivatives show potential protective effects on damaged cells and antiplatelet aggregation activities, with compound E1 being the most active antiplatelet aggregation agent.

Design, synthesis, and biological activities of novel Ligustrazine derivatives.

Novel Ligustrazine derivatives show lower EC(50) values for protecting ECV-304 cells damaged by hydrogen peroxide and better antiplatelet aggregation activities than Ligustrazine, with compounds 7a-c showing the highest potency.

Calcium Channel Blockers

Calcium channel blockers can effectively treat disorders associated with calcium channel activity, such as cardiovascular diseases like hypertension, congestive heart failure, arrhythmia, and angina.