Synthesis and pharmacological activity of 4-(4'-(chlorophenyl)-4-hydroxypiperidine) derivatives.

doi:10.1248/CPB.53.64

Paper

Synthesis and pharmacological activity of 4-(4'-(chlorophenyl)-4-hydroxypiperidine) derivatives.

Published 2005 · Z. Saify, N. Mushtaq, K. Khan

Chemical & pharmaceutical bulletin

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Abstract

A new series of 4-(4'-chlorophenyl)-4-hydroxypiperidine derivatives (2-5), substituted at nitrogen, were synthesized and tested as potential analgesic compounds as well as evaluated for their effect on hypotensive activity. Results showed that all the derivatives exhibit significant analgesic activity in male Wistar rats at a dose of 50 mg/kg of body weight after intramuscular injection, when tested by thermal stimuli (tail flick test). Pethidine was used as reference drug. Compounds 2, 3 and 5 produced reduction in blood pressure in normotensive rat.

Non-RCT

Animal Study

Study Snapshot

4-(4'-(chlorophenyl)-4-hydroxypiperidine) derivatives exhibit significant analgesic activity and reduced blood pressure in normotensive rats when administered intramuscularly.

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 pharmacological activity of 4-(4'-(chlorophenyl)-4-hydroxypiperidine) derivatives.

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References

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Compound 11 is a highly potent mu, kappa-, and delta-opioid antagonist with potential clinical utility as an appetite suppressant for weight loss.

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Highly potent and selective kappa-receptor agonists have been identified, with spirocyclic analogues showing exceptional potency.

Citations

Piperidine Derivatives: Synthesis, Pharmacological Evaluation and Insilico Approach of Novel Potential Analgesics in 4-amino Methyl Piperidine Series

HN58, a novel piperidine derivative, shows excellent analgesic activity and shows potential as a potent -opioid receptor inhibitor.

Synthesis, Pharmacological Evaluation and In-Silico Studies of Some Piperidine Derivatives as Potent Analgesic Agents

PP1, AMP5, and AMP6 show potent analgesic activity, with potential interaction with mu-opioid receptors and good binding affinity.

Characterisation of Plasmodium falciparum aspartic protease inhibition by piperidine derivatives

Nitrophenacyl derivatives of N-methyl-4-hydroxy piperidine show aspartic protease inhibitory activity against Plasmodium falciparum, with 1-methyl-1-(4'-nitrophenacyl)-4-hydroxypiperidinium bromide (3) being the most active at 1.0

Antinociceptive activity of some 1,4-substituted piperidine derivatives using tail flick method in mice

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Alkyl piperidine derivatives show varying analgesic activity and duration compared to pethidine, highlighting their potential therapeutic potential.

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