Synthesis of piperidine derivatives with a quinazoline ring system as potential antihypertensive agents.

doi:10.1248/CPB.34.1907

Paper

Synthesis of piperidine derivatives with a quinazoline ring system as potential antihypertensive agents.

Published May 25, 1986 · H. Takai, H. Obase, M. Teranishi

Chemical & pharmaceutical bulletin

Q3 SJR score

12

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0

Influential Citations

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Abstract

A series of piperidine derivatives with a 2-oxo-1, 2, 3, 4-tetrahydro-quinazoline or 2, 4-dioxo-1, 2, 3, 4-tetrahydroquinazoline ring at the 4-position were prepared and tested for antihypertensive activity. Among the compounds tested, 1-[2-hydroxy-2-(3, 4-methylenedioxyphenyl)ethyl]-4-(2, 4-dioxo-1, 2, 3, 4-tetrahydro-3-quinazolinyl)piperidine (20) and 1-[2-(4-chlorophenyl)-2-hydroxyethyl]-4-(2-oxo-1, 2, 3, 4-tetrahydro-3-quinazolinylmethyl)piperidine (30) produced relatively strong hypotension in the spontaneously hypertensive rat model.

Non-RCT

Animal Study

Study Snapshot

Piperidine derivatives with a quinazoline ring system show potential antihypertensive activity, with 1-[2-hydroxy-2-(3, 4-methylenedioxyphenyl)ethyl]-4-(2, 4-dioxo-1, 2, 3, 4-tetrahydro-3-

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 of piperidine derivatives with a quinazoline ring system as potential antihypertensive agents.

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References

Citations

A base-promoted synthesis of 3,4-dihydro-2(1H)-quinazolinones

This study developed a convenient base-promoted synthesis method for 3,4-dihydro-2(1H)-quinazolinones and multi-membered cyclic ureas under mild conditions, offering an alternative synthesis toolkit for cyclic ureas.

Insights into the structure activity relationship of nitrogen-containing heterocyclics for the development of antidepressant compounds: An updated review

Nitrogen-based heterocyclics play a crucial role in the development of antidepressant compounds, with potential for improved potency and reduced toxicity through multiple mechanisms.

Synthesis of substituted 3,4-dihydroquinazolinones via a metal free Leuckart–Wallach type reaction

This study developed a metal-free Leuckart-Wallach type reaction for preparing substituted 3,4-dihydroquinazolinones using readily-available starting materials, offering a flexible and efficient synthetic approach for biologically-active compounds.

The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase

K-756, a novel selective TNKS inhibitor, shows potential as a leading anticancer agent by inhibiting the Wnt/-catenin pathway in APC-mutant colon cancer cells and showing synergistic effects with gefitinib in non-small cell lung cancer cells.

Hydrophobically directed, catalyst-free, multi-component synthesis of functionalized 3,4-dihydroquinazolin-2(1H)-ones

The one-pot, catalyst-free reaction efficiently synthesizes functionalized 3,4-dihydroquinazolin-2(1H)-one derivatives with good to excellent antibacterial activity against both Gram positive and Gram negative bacteria.