Abstract

The goal of the study was to develop, synthesise, and characterise a novel 1,3,5-trisubstituted-2-pyrazolines derivative, as well as to assess its analgesic potential. The reaction of chalcone derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride yielded 1,3,5-tri-substituted-2-pyrazolines derivatives. The IR, 1HNMR, and mass spectrum analyses were used to characterise a total of sixteen substances. Analgesic activity of the proposed substances has been tested. The analgesic effect of the produced compounds was tested using two methods: the hot plate test technique and acetic acid induced writhing in mice. To compare the effectiveness, pentazocine and acetyl acetic acid were utilised as reference drugs. The hot plate test technique and acetic acid induced writhing in mice were used to assess the analgesic effect of the 16 produced chemical series A1-A8, and B1-B8. The evaluation's outcomes were viewed using Pentazocine and acetyl acetic acid as the standard drugs. In a 90-minute hot plate test, compounds A2 (10.30 s), A4 (9.45 s), A7 (11.65 s), and A8 (11.26 s) showed a delay in paw withdrawal latency time. Compounds B2 (9.10 s) and B7 (10.42 s) prolong the paw withdrawal latency time after 90 minutes in series B1-B8, reduce the pain feeling, and inhibit pain induced by heat methods. Compounds A2, A5, A6, A7, and A8 from Series A1-A8 showed 83.00, 76.01, 80.34, 86.99, 88.15 percent inhibition, substantially (p0.05 and p0.001, respectively), and decreased the number of wriths caused by 0.6 percent acetic acid at a dosage of 10 mg/kg. Acetylsalicylic acid (10 mg/kg) appears to be more successful in lowering the number of wriths, with a 99.0% reduction in the number of wriths (p0.001). B1, B3, and B4 have the least amount of active activity. These all finding suggest that these synthesized compounds have the potential as analgesic agent.

Highlights

  • Any member of the category of medications used to induce analgesia is referred to as an analgesic. [1] Analgesic medications affect the peripheral and central nerve systems in a variety of ways

  • B1, B3, and B4 have the least amount of active activity. These all finding suggest that these synthesized compounds have the potential as analgesic agent

  • Pentazocine and acetyl acetic acid were utilised as reference drugs

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Summary

Introduction

Any member of the category of medications used to induce analgesia (pain alleviation) is referred to as an analgesic. [1] Analgesic medications affect the peripheral and central nerve systems in a variety of ways. Any member of the category of medications used to induce analgesia (pain alleviation) is referred to as an analgesic. [1] Analgesic medications affect the peripheral and central nerve systems in a variety of ways. An analgesic is a medicine that reduces pain selectively by acting in the central nervous system (CNS) or on peripheral pain mechanisms without affecting consciousness. Substitutions may be synthesised, which undergo a cyclo-addition process with substituted hydrazine to provide desirable 1,3,5-tri substituted pyrazole derivatives. Several chalcone derivatives were synthesised and employed as intermediates in the synthesis of [1,3,5] tri substituted pyrazole in the current work. The objective of the paper was to design, synthesis and characterization of new 1,3,5trisubstituted-2-pyrazolines derivative and evaluate for analgesic potential

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