The Search for Biologically Active Compounds in the Series of N-ethoxyethylpiperidine Derivatives

Issayeva, U. B.; Akhmetova, G. S.; Datkhayev, Ubaidilla; Omyrzakov, M; Praliyev, K. D.; Ross, Samir A.

doi:10.18321/ectj822

Cited by 4 publications

(2 citation statements)

References 12 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Of these, the inclusion complexes of kazcaine and AEPP can be considered the most promising. Moreover, recently obtained fluorine derivatives of kazcaine have shown unexpected antimicrobial activity [ 43 , 44 ].…”

Section: Discussionmentioning

confidence: 99%

Comparative Analysis of the Structure and Pharmacological Properties of Some Piperidines and Host–Guest Complexes of β-Cyclodextrin

Kemelbekov,

Volynkin,

Zhumakova

et al. 2024

Molecules

View full text Add to dashboard Cite

Pain and anesthesia are a problem for all physicians. Scientists from different countries are constantly searching for new anesthetic agents and methods of general anesthesia. In anesthesiology, the role and importance of local anesthesia always remain topical. In the present work, a comparative analysis of the results of pharmacological studies on models of the conduction and terminal anesthesia, as well as acute toxicity studies of the inclusion complex of 1-methyl-4-ethynyl-4-hydroxypiperidine (MEP) with β-cyclodextrin, was carried out. A virtual screening and comparative analysis of pharmacological activity were also performed on a number of the prepared piperidine derivatives and their host–guest complexes of β-cyclodextrin to identify the structure–activity relationship. Various programs were used to study biological activity in silico. For comparative analysis of chemical and pharmacological properties, data from previous works were used. For some piperidine derivatives, new dosage forms were prepared as beta-cyclodextrin host–guest complexes. Some compounds were recognized as promising local anesthetics. Pharmacological studies have shown that KFCD-7 is more active than reference drugs in terms of local anesthetic activity and acute toxicity but is less active than host–guest complexes, based on other piperidines. This fact is in good agreement with the predicted results of biological activity.

show abstract

Section: Discussionmentioning

confidence: 99%

Comparative Analysis of the Structure and Pharmacological Properties of Some Piperidines and Host–Guest Complexes of β-Cyclodextrin

Kemelbekov,

Volynkin,

Zhumakova

et al. 2024

Molecules

View full text Add to dashboard Cite

show abstract

“…The presence of a fluorine atom in the molecule of organic compounds increases their bioavailability, metabolic stability, lipophilicity, and also improves the ability of these substances to interact with the target proteins ( 21 ). As the study objects, m- and o- fluorobenzoate esters of 1-(2-ethoxyethyl-4-ethynylpiperidin-4-ols) were synthesized, which was previously described in the study of these compounds as potential antimicrobial agents ( 22 ). The synthesized fluorobenzoates are fluorine analogues of Kazcaine (1-(2-ethoxyethyl-4-ethynyl-4-benzoyloxypiperidine hydrochloride), which has shown excellent properties as a local anesthetic ( 19 , 20 ).…”

Section: Methodsmentioning

confidence: 99%

Experimental study of local anesthetic and antiarrhythmic activities of fluorinated ethynylpiperidine derivatives

Satbayeva,

Zhumakova,

Khaiitova

et al. 2024

Braz J Med Biol Res

View full text Add to dashboard Cite

The chemical structure of piperidine has a unique ability to combine with other molecular fragments. This fact makes it possible to actively use it as an effective basis for the creation of new drug-like substances. Thus, the aim of the current investigation was to study the acute toxicity, local anesthetic potency, and antiarrhythmic activity of the two new synthesized piperidine derivatives under laboratory codes LAS-286 and LAS-294 (local anesthetic substances). The Bulbring & Wajda animal model and method of determining the nociception threshold during electrical stimulation was used to investigate the action of the substance during infiltration anesthesia. An antiarrhythmic activity was observed by the aconitine-induced rat arrhythmia model. Additionally, these compounds were studied in relation to molecular docking to delineate the structure-activity relationships. The tested piperidine derivatives had a low toxicity in the subcutaneous and intravenous administration routes. The experimental results showed a higher prolonged and pronounced local anesthetic activity for LAS-286 at a 0.5% concentration, compared to the reference preparations. The low dosage of 0.1 mg/kg of LAS-294 demonstrated a pronounced preventive antiarrhythmic effect in 90% of cases on the development of mixed arrhythmia, caused by aconitine. The results of molecular docking confirmed a higher binding affinity of the tested piperidines with the Na v 1.4 and Na v 1.5 macromolecules. The results of the present study are very promising, because these piperidines have shown a high biological activity, which can suggest a potential therapeutic application in the future.

show abstract

Phytochemical Studies, Anti-Oxidant and Anti- Inflammatory Properties of Four Medicinal Plants

Sharma,

Goel

2023

JEOH

View full text Add to dashboard Cite

Rheumatoid arthritis, a chronic autoimmune disorder, is characterized by polyarthralgia and joint dysfunction resulting from autoimmune responses that target self-neoepitopes. These attacks lead to the activation of macrophages and other defense cells. By identifying these self-epitopes as biomarkers in RA, researchers have gained valuable insights into the disease’s pathogenesis. Over the years, research has focused on investigating the potential of medicinal plants as antiinflammatory agents. In this study, a hydroethanolic extract of Saraca asoca, Ficus benghalensis, Chenopodium album, and Nyctanthes arbor-tristis leaves was prepared by Soxhlet apparatus. Various concentrations of extracts were utilized to assess phytochemical analysis, GC-MS, in-vitro anti-oxidant, and anti-inflammatory activities. The highest scavenging potential was exhibited by Chenopodium album, as assessed by the DPPH assay (90.32 ± 3.2 %) and H2O2 (86.00 ± 1.94 %). Similarly, the Nyctanthes arbor-tristis showed (92.23 ± 0.83 %) inhibition in membrane stabilization assay, and (91.49 ± 1.03 %) in protein denaturation inhibition capacity. GCMS analysis showed various phytoconstituents in extracts. In order to confirm its therapeutic potential for treating RA, Nyctanthes arbor-tristis may be a better drug candidate that needs to be further researched for mechanistic studies.

show abstract

The Search for Biologically Active Compounds in the Series of N-ethoxyethylpiperidine Derivatives

Cited by 4 publications

References 12 publications

Comparative Analysis of the Structure and Pharmacological Properties of Some Piperidines and Host–Guest Complexes of β-Cyclodextrin

Comparative Analysis of the Structure and Pharmacological Properties of Some Piperidines and Host–Guest Complexes of β-Cyclodextrin

Experimental study of local anesthetic and antiarrhythmic activities of fluorinated ethynylpiperidine derivatives

Phytochemical Studies, Anti-Oxidant and Anti- Inflammatory Properties of Four Medicinal Plants

Contact Info

Product

Resources

About