Synthesis, crystal structures, fluorescence and xanthine oxidase inhibitory activity of pyrazole-based 1,3,4-oxadiazole derivatives

Qi, De-Qiang; Yu, Chuanming; You, Jingsong; Yang, Guanghui; Wang, Xuejie; Zhang, Yiping

doi:10.1016/j.molstruc.2015.07.067

Cited by 25 publications

(12 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Pyrazoles were also found to possess inhibitory activities against xanthine oxidase, cyclooxygenase, and alkaline phosphatases [5][6][7]. Particular substituents at the pyrazole provide additional biological activities [8,9].…”

Section: Discussionmentioning

confidence: 99%

Crystal structure of methyl 1-(4-fluorobenzyl)-3-phenyl-1H-pyrazole-5-carboxylate, C₁₈H₁₅FN₂O₂

Sheng-Yue

You

Zhang

et al. 2017

Zeitschrift Für Kristallographie - New Crystal Structures

Self Cite

View full text Add to dashboard Cite

show abstract

Section: Discussionmentioning

confidence: 99%

Crystal structure of methyl 1-(4-fluorobenzyl)-3-phenyl-1H-pyrazole-5-carboxylate, C₁₈H₁₅FN₂O₂

Sheng-Yue

You

Zhang

et al. 2017

Zeitschrift Für Kristallographie - New Crystal Structures

Self Cite

View full text Add to dashboard Cite

show abstract

“…The XO inhibitory activity of as eries of 1,3,4-oxadiazole derivatives 171 was tested by Qi et al [122] The authors concluded that further optimization was neededf or the two most promising compounds, althought hey were less active than allopurinol. An itro group at positionRg enerated a compound with an IC 50 value of 72.4 mm,a nd ac yano group at the same positiong enerated ac ompound with an IC 50 of 75.6 mm,w hile allopurinol was determined to have an IC 50 of 2.3 mm.…”

Section: Zhang Et Al In 2017mentioning

confidence: 99%

“…The XO inhibitory activity of a series of 1,3,4‐oxadiazole derivatives 171 was tested by Qi et al . The authors concluded that further optimization was needed for the two most promising compounds, although they were less active than allopurinol.…”

Section: Non‐purine‐like Inhibitors Of Xomentioning

confidence: 99%

Inhibitors of Xanthine Oxidase: Scaffold Diversity and Structure‐Based Drug Design

2019

View full text Add to dashboard Cite

Xanthine oxidase (XO) is the enzyme responsible for the catabolism of purines and their conversion into uric acid. XO is thus the target for the treatment of hyperuricemia and gout. For more than 50 years the only XO inhibitor drug available on the market was the purine analogue allopurinol. In the last decade there has been a resurgence in the search for new inhibitors of XO, as the activity of XO and hyperuricemia have also been associated with a variety of conditions such as diabetes, hypertension, and other cardiovascular diseases. In recent years the non‐purine inhibitor febuxostat was approved in Europe and the USA for the treatment of hyperuricemia. This drug was followed by another XO inhibitor called topiroxostat. This review discusses the molecular structures and activities of the multiple classes of inhibitors that have been developed since the discovery of allopurinol, with a brief review of the molecular interactions between inhibitors and XO active site residues for the most important molecules. The challenges ahead for the discovery of new inhibitors of XO with novel chemical structures are discussed.

show abstract

“…Scheme 18:-Qi DQ, et al, [13] (2015) were designed and synthesised a series of pyrazole-based 1, 3, 4-oxadiazole derivatives (scheme: 19). The fluorescence properties of all the compounds were analysed in dimethyl sulfoxide media and were evaluated for their n vitro inhibitory activity against commercial enzyme xanthine oxidase (XO) by measuring the formation of uric acid from xanthine.…”

Section: Ar= Aryl Halidesmentioning

confidence: 99%

Synthesis and Biological Activities of 1, 3, 4-Oxadiazole Derivatives: A Review of Literature.

Baijika¹

2018

IJAR

View full text Add to dashboard Cite

Synthesis, crystal structures, fluorescence and xanthine oxidase inhibitory activity of pyrazole-based 1,3,4-oxadiazole derivatives

Cited by 25 publications

References 35 publications

Crystal structure of methyl 1-(4-fluorobenzyl)-3-phenyl-1H-pyrazole-5-carboxylate, C₁₈H₁₅FN₂O₂

Crystal structure of methyl 1-(4-fluorobenzyl)-3-phenyl-1H-pyrazole-5-carboxylate, C₁₈H₁₅FN₂O₂

Inhibitors of Xanthine Oxidase: Scaffold Diversity and Structure‐Based Drug Design

Synthesis and Biological Activities of 1, 3, 4-Oxadiazole Derivatives: A Review of Literature.

Contact Info

Product

Resources

About

Synthesis, crystal structures, fluorescence and xanthine oxidase inhibitory activity of pyrazole-based 1,3,4-oxadiazole derivatives

Cited by 25 publications

References 35 publications

Crystal structure of methyl 1-(4-fluorobenzyl)-3-phenyl-1H-pyrazole-5-carboxylate, C18H15FN2O2

Crystal structure of methyl 1-(4-fluorobenzyl)-3-phenyl-1H-pyrazole-5-carboxylate, C18H15FN2O2

Inhibitors of Xanthine Oxidase: Scaffold Diversity and Structure‐Based Drug Design

Synthesis and Biological Activities of 1, 3, 4-Oxadiazole Derivatives: A Review of Literature.

Contact Info

Product

Resources

About

Crystal structure of methyl 1-(4-fluorobenzyl)-3-phenyl-1H-pyrazole-5-carboxylate, C₁₈H₁₅FN₂O₂

Crystal structure of methyl 1-(4-fluorobenzyl)-3-phenyl-1H-pyrazole-5-carboxylate, C₁₈H₁₅FN₂O₂