Design and environmentally benign synthesis of novel thiophene appended pyrazole analogues as anti-inflammatory and radical scavenging agents: Crystallographic , in silico modeling, docking and SAR characterization

Prabhudeva, M. G.; Srinivasan, Bharath; Kumar, A. Dileep; Naveen, S.; Lokanath, N.K.; Mylarappa, B. N.; Kumar, K. Ajay

doi:10.1016/j.bioorg.2017.06.004

Cited by 37 publications

(12 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The interaction and compact overlap of thiophene–pyrazole conjugate (compound 47 ) with soluble human PLA 2 (an important enzyme in arachidonic acid cascade) seem to confer an additional pharmacological advantage. The site of interaction appears to be between the backbone carbonyl oxygens of Gly45, Gly47, Tyr43, and the side‐chain carboxylate group of Asp64 [43].…”

Section: Preclinical and Mechanistic Studies Of Pyrazoles Derivativesmentioning

confidence: 99%

Development of pyrazole derivatives in the management of inflammation

Turones

Martins

Moreira

et al. 2020

Fundamemntal Clinical Pharma

View full text Add to dashboard Cite

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.

show abstract

Section: Preclinical and Mechanistic Studies Of Pyrazoles Derivativesmentioning

confidence: 99%

Development of pyrazole derivatives in the management of inflammation

Turones

Martins

Moreira

et al. 2020

Fundamemntal Clinical Pharma

View full text Add to dashboard Cite

show abstract

“…Pyrazole is also an important scaffold in many natural products. Pyrazole containing compounds are usually associated with activities such as antifungal [5], anti-inflammatory [6], insecticidal [7] and antiviral [8] properties. Substituted pyrazoles showed selective anti-proliferative actions on many human cancer cells and hold promise as inhibitors of cellular proliferation [9][10][11][12][13].…”

Section: Introductionmentioning

confidence: 99%

Copper(II) ions mediated crystal formation of 3-(3-hydroxy phenyl)-1-phenyl-1h-pyrazole- 4-carbaldehyde

Banpurkar¹,

Wazalwar²,

Perdih³

2021

Bull. Chem. Soc. Eth.

View full text Add to dashboard Cite

Schiff base obtained from 3-hydroxyacetophenone and phenylhydrazine was subjected to Vilsmeier-Haack reaction to obtain 3-(3-hydroxyphenyl)-1-phenyl-1H-pyrazole-4-carbaldehyde (2). Successful formation of crystals of 2 was achieved using copper ions (Cu2+) as template. Present paper reports study of spectroscopic characterization and single-crystal X-ray study of 2. Hydrogen bonding network between 2 and water molecules enable the formation of 2D layer along ab-plane supported also by π···π stacking interactions of parallel molecules in head-to-head fashion. KEY WORDS: Cu2+ assisted crystal growth, Pyrazole-4-carbaldehyde, X-ray crystal study, Hydrogen bonding study Bull. Chem. Soc. Ethiop. 2020, 34(3), 589-596. DOI: https://dx.doi.org/10.4314/bcse.v34i3.13

show abstract

“…Moreover, pyrazole-based heterocycles as thiophenes, 2-alkyloxypyridines and thieno [2,3-d]pyrimidines have been given more attention due to their useful therapeutic fields including, muscle relaxing, antitumor, anti-depressant, antimicrobial, antidiabetic, antitubercular, antioxidant, HIV reverse transcriptase inhibitors and also possess significant vasodilation activities [11][12][13][14][15][16][17]. They also demonstrated strong anti-inflammatory action with low GIT toxicity and analgesic impacts [18][19][20][21][22][23][24]. In the same way, and in the continuing work on synthesis of biologically active heterocycles based pyrazoles [25][26][27][28][29], we focused in this study on designing of new molecules carrying pyrazole substituents as hybrids with various heterocycles aiming to get potent candidates with analgesic properties.…”

Section: Introductionmentioning

confidence: 99%

Novel synthesis of pyrazole-containing thiophene, 2-alkyloxy-pyridine and thieno[2,3-d]pyrimidine scaffolds as analgesic agents

Khalifa¹,

Fahmy²,

Nossier³

et al. 2019

Bull. Chem. Soc. Eth.

View full text Add to dashboard Cite

A group of trisubstituted pyrazoles containing thiophen, 2-alkyloxypyridine and thieno[2,3d]pyrimidine heterocycles were synthesized in a study for possible analgesic agents. The desired products were obtained by reaction of 2-((1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazol-4-yl)methylene)malononitrile with sulfur in presence of TEA, followed by treatment with different reagents. Newer products were examined for their analgesic properties, among them, analog 7 showed significant analgesic effects in comparison with reference medicines activity.

show abstract

Design and environmentally benign synthesis of novel thiophene appended pyrazole analogues as anti-inflammatory and radical scavenging agents: Crystallographic , in silico modeling, docking and SAR characterization

Cited by 37 publications

References 22 publications

Development of pyrazole derivatives in the management of inflammation

Development of pyrazole derivatives in the management of inflammation

Copper(II) ions mediated crystal formation of 3-(3-hydroxy phenyl)-1-phenyl-1h-pyrazole- 4-carbaldehyde

Novel synthesis of pyrazole-containing thiophene, 2-alkyloxy-pyridine and thieno[2,3-d]pyrimidine scaffolds as analgesic agents

Contact Info

Product

Resources

About