Piperazine: A Promising Scaffold with Analgesic and Anti-inflammatory Potential

Jain, Akash; Chaudhary, Jasmine; Khaira, Harpreet; Chopra, Bhawna; Dhingra, Ashwani Kumar

doi:10.1055/a-1323-2813

Cited by 34 publications

(13 citation statements)

References 67 publications

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“…A large group of piperazine derivatives has a central effect [6,13], for example, it acts on serotonin [42,64,65], dopamine [16,49] and even on cannabinoid [40] receptors, affects the activity of MAO (monoamine oxidase) [49,62], therefore represents a potential class of drugs that have antipsychotic [11], antidepressant [36,63], in some cases anxiolytic activity [13,19]. In some cases, their analgesic and anti-inflammatory effects are described [26]. There are works describing their antiarrhythmic properties [3,4,33,51,52].…”

Section: Results Of a Study Of The Local Anaesthetic Activity Of Pipe...mentioning

confidence: 99%

“…Currently, piperazine derivatives are one of the most popular heterocyclic compounds used for the development of new candidate drugs. In particular, literary sources reveal the analgesic potential of piperazine derivatives [26,58,66]. In recent years, studies have revealed the presence of antinociceptive, locally anaesthetic, analgesic types of activity in modified piperazine derivatives.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Experimental Study of the Local Anesthetic Activity of New Modified Piperazine Derivatives

KHAIITOVA¹

2023

FARMACIA

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N-substituted piperazines, an important class of compounds with different pharmacological activities were taken as the basic starting object for the synthesis and study of α-aminophosphonates. The objective of the study was the synthesis, analysis of biological effects (toxicity and local anaesthetic activity) of some new piperazine derivatives, and the evaluation of their potential pharmacological effects. The new piperazine derivatives were coded as LAS-276, LAS-277, LAS-278, where LAS is a local anaesthetic substance. The compounds were synthesized under the conditions of the Kabachnik-Fields reaction. Their acute toxicity in mice, the local anaesthetic activity in a regional and infiltration anaesthesia models were studied, and their estimated pharmacological activity was analysed using the online PASS (Prediction of Activity Spectra for Substances) program. In a series of experiments the administration of high doses of the studied compounds has not caused death of laboratory animals. The study of local anaesthetic activity in the infiltration anaesthesia model showed varying degrees of activity. The compounds showed moderate activity on the regional anaesthesia model. The PASS analysis revealed a very high probability of thrombolytic, anticoagulant, antisclerotic effects and stimulation of endothelin receptors. The implemented studies revealed the low toxicity, moderate local anaesthetic activity of the studied piperazine compounds. There is also a high probability of their thrombolytic activity, which requires further research. RezumatPiperazinele N-substituite sunt o clasă importantă de compuși cu activitate farmacologică ce stau la baza sintezei și studiul αaminofosfonaților. Obiectivele studiului au fost sinteza, analiza efectelor biologice (toxicitate și activitate anestezică locală) și evaluarea efectelor farmacologice ale noilor derivați de piperazină. Compușii au fost sintetizați în condițiile reacției Kabachnik-Fields. Apoi s-a studiat toxicitatea lor după administrarea în doză unică la șoareci, activitatea anestezică locală într-o anestezie regională și modele de infiltrație. Activitatea lor farmacologică a fost evaluată folosind programul online PASS (Predicția Spectrelor de Activitate pentru Substanțe). Într-o serie de experimente, administrarea de doze mari din compușii studiați nu a provocat moartea animalelor de laborator. Studiul activității anestezice locale în modelul de anestezie prin infiltrare a arătat grade variate de activitate. Compușii au prezentat activitate moderată în modelul de anestezie regională. Analiza PASS a relevat o probabilitate foarte mare de efecte trombolitice, anticoagulante, antisclerotice și de stimulare a receptorilor de endotelină. Studiile implementate au evidențiat toxicitatea scăzută, precum și activitatea anestezică locală moderată a compușilor piperazinici studiați. Există, de asemenea, o probabilitate mare a activității lor trombolitice, ceea ce necesită cercetări suplimentare.

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Section: Results Of a Study Of The Local Anaesthetic Activity Of Pipe...mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and Experimental Study of the Local Anesthetic Activity of New Modified Piperazine Derivatives

KHAIITOVA¹

2023

FARMACIA

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“…Most importantly, piperazine is an essential heterocyclic motif in many biologically active compounds with various pharmacological activities. [19][20][21][22][23][24][25][26][27] For example, clozapine 1 is strongly sedative and has muscle-relaxant properties, amoxapine 2 has antidepressant activity, trimetazidine 3 is an antischemic agent and cyclizine 4 is used to treat nausea and vomiting 28,29 (Figure 1). Structurally, piperazine has a six-membered saturated ring with two nitrogen atoms at 1-and 4-positions.…”

Section: Introductionmentioning

confidence: 99%

Polyketopiperazines: triketopiperazines, tetraketopiperazines synthesis, reactions, bioactivities and applications

sharafeldin¹

2022

Arkivoc

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Several polyketopiperazines represent the simplest heterocyclic compounds found in nature, acting as a vital base-structure for many bioactive compounds. They are widely distributed in microorganisms, food, and beverages with diverse bioactivities, such as antiviral, anticancer, antioxidant, and neuroprotective properties. Focusing on triketopiperazines and tetraketopiperazines; triketopiperazines possess important biological properties and used for production of the valuable molecular scaffolds in synthetic biology, whereas tetraketopiperazines are economically beneficial for chemical engineering. Noteworthy, they have extra-rigid conformations and are more resistant to degradation by enzymes. Therefore, they represent an interesting subclass of heterocycles with high potential to be used in the production of new effective therapeutic motif and sustainable energy storage structures.

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“…Hence, there is a need for a continual search for novel compounds with good potency and better selectivity indices. Analogs of different heterocyclic scaffolds such as pyrimidine, [ 6 ] imidazole, [ 7 ] pyrrole, [ 8 ] piperazine, [ 9 ] and oxazole [ 10 ] have demonstrated varying medicinal properties including anticancer activity. Particularly, the oxazole motif has been repeatedly found in various anticancer molecules.…”

Section: Introductionmentioning

confidence: 99%

“…Analogs of different heterocyclic scaffolds such as pyrimidine, [6] imidazole, [7] pyrrole, [8] piperazine, [9] and oxazole [10] have demonstrated varying medicinal properties including anticancer activity.…”

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confidence: 99%