Synthesis and bioactivities of some new 1H-pyrazole derivatives containing an aryl sulfonate moiety

Pyrazoles are considered privileged scaffolds in medicinal chemistry. Previous reviews have discussed the importance of pyrazoles and their biological activities; however, few have dealt with the chemistry and the biology of heteroannulated derivatives. Therefore, we focused our attention on recent topics, up until 2020, for the synthesis of pyrazoles, their heteroannulated derivatives, and their applications as biologically active moieties. Moreover, we focused on traditional procedures used in the synthesis of pyrazoles.

show abstract

“…Kendre et al reported some 1 H -pyrazole derivatives containing aryl sulfonate moieties 266 with anti-inflammatory effects ( Figure 16 ) [ 177 ].…”

Section: Biological Activitiesmentioning

confidence: 99%

Substituted Pyrazoles and Their Heteroannulated Analogs—Recent Syntheses and Biological Activities

et al. 2021

View full text Add to dashboard Cite

show abstract

“…The synthesis of thiazolopyrimidines 4a-l was carried out by an efficient and versatile synthetic route as outlined in Scheme 2. In the first stage, the important substrates 2-(3dimethylamino)acryloyl)phenyl 4-methylbenzene sulfonates 3a-d were prepared following our previous protocol [24] and 2,3-dihydro-4-phenylthiazol-2-amines 2a-d were prepared from commercially available 2-amino-4-phenyl thiazoles 1a-d. 2-Amino-4-phenyl thiazole 1a on treating with lithium aluminium hydride (LiAlH4) in tetrahydrofuran gives 2,3-dihydro-4phenylthiazol-2-amine 2a in 90% yield at room temperature. The structure of this compound was confirmed by spectroscopic methods.…”

Section: Chemistrymentioning

confidence: 99%

Antimicrobial and Anti-Inflammatory Activity Studies of Novel Thiazolopyrimidines

Kendre¹,

Bhusare²,

Hardas³

2020

AJPTR

Self Cite

View full text Add to dashboard Cite

Novel thiazolopyrimidine derivatives (4a-l) were efficiently synthesized via the cyclocondensation reactions of 2-(3-dimethylamino) acryloyl) phenyl 4-methylbenzene sulfonates with 2,3-dihydro-4-phenylthiazol-2-amines under microwave irradiation in ethanol catalyzed by iodine and the synthesized compounds were evaluated for their in vitro antimicrobial and antiinflammatory activities. Among the newly synthesized compounds, 4d, 4h and 4l have exhibited potent antibacterial activity where as other derivatives 4b and 4j have showed moderate activity in comparison to standard drug amphcillin. The derivatives, 4d and 4l have displayed potent antifungal activity when their activity data was compared with standard drug norcadine. Some of the selected compounds were also screened for their anti-inflammatory activity and the results are compared with standard drug indomethacin. Among the derivatives, 4j possessed potent antiinflammatory activity while 4b, 4f and 4k have exhibited moderate activity.

show abstract

“…Kumar et al synthesized some new pyrimidine pyrazole heterocycles [48]. Following antifungal evaluation, compounds (18) and (19) showed synergy with standard drug ketoconazole at 1:8 (6.25:50.0 μg/ml) and 1:4 (25:100 μg/ml) against Aspergillus fumigatus (ITCC 4517) and A. fumigatus (VPCI 190/96), respectively.…”

Section: Research In 2014mentioning

confidence: 99%

“…Recently, researcher's attention has been paid to heterocycles containing nitrogen atom, particularly pyrazoles and their derivatives [10]. They have been found to denote versatile biological activities such as monoamine oxidase inhibitor [11,12], antihepatotoxicity [13,14], antileishmanial [15][16][17], anti-inflammatory [18][19][20], antiproliferative [21], tissue non-specific alkaline phosphatase inhibitor [22], cyclin-dependent kinase inhibitor [23], anticancer [24][25][26][27], antimicrobial [28][29][30], and antioxidant [31][32][33]. Development of novel chemical structures of pyrazole derivatives is currently a trending topic due to their wonderful biological actions [34][35][36][37].…”

Section: Introductionmentioning

confidence: 99%

A Recent Update: Antimicrobial Agents Containing Pyrazole Nucleus

Ardiansah

2018

Asian J Pharm Clin Res

View full text Add to dashboard Cite

Objective: In this review, we report antimicrobial candidates containing pyrazole nucleus integrated with various functionalities.Methods: research results by numerous scientists have been summarized from international journals indexed in reputed database such as Scopus and Web of Science.Results: Pyrazole derivatives are much of interest as potent bioactive molecules. They have shown large bioactivities especially antimicrobial performance against broad spectrum of bacterial strains.Conclusion: Several designed pyrazole derivates possessed good to superior antimicrobial activities.

show abstract

Synthesis and bioactivities of some new 1H-pyrazole derivatives containing an aryl sulfonate moiety

Cited by 20 publications

References 18 publications

Substituted Pyrazoles and Their Heteroannulated Analogs—Recent Syntheses and Biological Activities

Substituted Pyrazoles and Their Heteroannulated Analogs—Recent Syntheses and Biological Activities

Antimicrobial and Anti-Inflammatory Activity Studies of Novel Thiazolopyrimidines

A Recent Update: Antimicrobial Agents Containing Pyrazole Nucleus

Contact Info

Product

Resources

About