Pyrazole Bearing Molecules as Bioactive Scaffolds: A Review

Aziz, Hira; Zahoor, Ameer Fawad; Ahmad, Sajjad

doi:10.4067/s0717-97072020000104746

Cited by 41 publications

(24 citation statements)

References 40 publications

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“…The chemical structure and biological targets are important clues for identifying pyrazole derivatives with potential anti‐inflammatory activity [23,86,87]. Over the years, the attachment of important functional groups to the pyrazole ring was used to create derivatives [22,88,89]. The analysis of chemical structures has enriched our comprehension of the modifications that enhance or reduce either therapeutic or toxic effects [89–96].…”

Section: Structure–activity Relationship (Sar) Of Pyrazole Derivativesmentioning

confidence: 99%

“…Over the years, the attachment of important functional groups to the pyrazole ring was used to create derivatives [22,88,89]. The analysis of chemical structures has enriched our comprehension of the modifications that enhance or reduce either therapeutic or toxic effects [89–96]. Some of the pyrazole derivatives shown in Table I possess a variety of biological effects (reduction of inflammatory or pain response) that are related to effective dose (ED), COX selectivity index (SI), and half‐maximal inhibitory concentration (IC50).…”

Section: Structure–activity Relationship (Sar) Of Pyrazole Derivativesmentioning

confidence: 99%

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Development of pyrazole derivatives in the management of inflammation

Turones

Martins

Moreira

et al. 2020

Fundamemntal Clinical Pharma

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The therapeutic limitations and poor management of inflammatory conditions are anticipated to impact patients negatively over the coming decades. Following the synthesis of the first pyrazole—antipyrine in 1887, several other derivatives have been screened for anti‐inflammatory, analgesic, and antipyretic activities. Arguably, the pyrazole ring, as a major pharmacophore and central scaffold partly, defines the pharmacological profile of several derivatives. In this review, we explore the structural–activity relationship that accounts for the pharmacological profile of pyrazole derivatives and highlights future research perspectives capable of optimizing current advancement in the search for safe and efficacy anti‐inflammatory drugs. The flourishing research into the pyrazole derivatives as drug candidates has advanced our understanding of inflammation‐related diseases and treatment.

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Section: Structure–activity Relationship (Sar) Of Pyrazole Derivativesmentioning

confidence: 99%

Section: Structure–activity Relationship (Sar) Of Pyrazole Derivativesmentioning

confidence: 99%

Development of pyrazole derivatives in the management of inflammation

Turones

Martins

Moreira

et al. 2020

Fundamemntal Clinical Pharma

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“…780/PO/Re/S/03/ CPCSEA and Letter reference number is Animal ethical committee RKDFCP/IAEC/2020/01). Rats in groups of 34 were administered orally with different doses by the staircase method, starting from 10 mg/kg and increasing dose by a factor 1.5, if there was no mortality [12] and decreasing subsequent dose by a factor 0.7 in case there was mortality. [13] Least tolerated (100% mortality) and most tolerated (0% mortality) were determined by hit and trial method.…”

Section: Analgesic Activitymentioning

confidence: 99%

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2020

IJPBA

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Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2-pyrazolines derivative and to evaluate for analgesic potential. Materials and Methods: The 1,3,5-trisubstituted-2-pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with 4-hydrazinylbenzene sulfonamide hydrochloride and phenyl hydrazine hydrochloride. Total 16 compounds have been synthesized and characterized by the IR, 1HNMR, and mass spectral analysis. Proposed compounds have been evaluated for analgesic activity. The synthesized compounds also evaluated for the analgesic activity by the following two methods, that is, hot plate test method and acetic acid induced writhing in mice. Pentazocine and acetyl acetic acid were used as standard drug for compare the efficacy. Results and Discussion: The analgesic activity of the 16 synthesized compound series A1-A8, and B1-B8 has been evaluated using hot plate test method and acetic acid induced writhing in mice. The results of the evaluation have been viewed by taking pentazocine and acetyl acetic acid as the standard drug. In hot plate test, series A1-A8, shown delay the paw withdrawal latency time for compound A2 (10.30 s), A4 (9.45 s), A7 (11.65 s), and A8 (11.26 s) after 90 min. In series, B1-B8 shown delay the paw withdrawal latency time for compound B2 (9.10 s) and B7 (10.42 s) after 90 min, inhibit the pain sensation, and inhibit pain produced by thermal means. Synthesized compounds of series A1-A8, compounds A2, A5, A6, A7, and A8 were shown 83.00, 76.01, 80.34, 86.99, and 88.15 were shown percent inhibition, significantly (p<0.05 and p<0.001, respectively) and reduced the number of wriths induced by 0.6% acetic acid at the dose of 10 mg/kg. Acetylsalicylic acid (10 mg/kg) appears to be better effective in reducing the number of wriths, it significantly (P < 0.001) reduced the number of wriths by 99.0%. The compounds B1, B3, and B4 have shown least active activity. These all finding suggest that these synthesized compounds have the potential as analgesic agent. Conclusion: The 1,3,5-pyrazoline derivatives has been successfully synthesized and evaluated for analgesic activity of mice model and results data indicate that compounds A2,

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“…The substitutions, additions, removal, or fusion of different functional groups in the pyrazole ring are key to the synthesis of lead compounds that are effective against emerging and complex diseases ( Faisal et al, 2019 ; Aziz et al, 2020 ; Ramsay et al, 2018 ; Benek et al, 2020 ; He et al, 2016 ). Pharmacological characterization of these analogs will benefit from our comprehension of the functional group modifications on the central pyrazole ring ( Figure 2 ).…”

Section: Introductionmentioning

confidence: 99%

Heterocyclic Compounds: Pharmacology of Pyrazole Analogs From Rational Structural Considerations

et al. 2021

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Low quality of life and life-threatening conditions often demand pharmacological screening of lead compounds. A spectrum of pharmacological activities has been attributed to pyrazole analogs. The substitution, replacement, or removal of functional groups on a pyrazole ring appears consistent with diverse molecular interactions, efficacy, and potency of these analogs. This mini-review explores cytotoxic, cytoprotective, antinociceptive, anti-inflammatory, and antidepressant activities of some pyrazole analogs to advance structure-related pharmacological profiles and rational design of new analogs. Numerous interactions of these derivatives at their targets could impact future research considerations and prospects while offering opportunities for optimizing therapeutic activity with fewer adverse effects.

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Pyrazole Bearing Molecules as Bioactive Scaffolds: A Review

Cited by 41 publications

References 40 publications

Development of pyrazole derivatives in the management of inflammation

Development of pyrazole derivatives in the management of inflammation

Untitled

Heterocyclic Compounds: Pharmacology of Pyrazole Analogs From Rational Structural Considerations

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