Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity

Bansal, Sumit; Bala, Manju; Kumar, Sunita; Choudhary, Shivani; Bhattacharya, Shoumyo; Bhardwaj, Varun; Singla, Sumit; Joseph, Alex

doi:10.1016/j.ejmech.2014.04.045

Cited by 92 publications

(44 citation statements)

References 36 publications

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“…Prostaglandins are produced from arachidonic acid (AA) through the catalysis of endoperoxide synthase or cyclooxygenase (COX) (Bansal et al, 2014). Arachidonic acid is released upon the destruction of phospholipids in the cell membrane.…”

Section: Inhibitory Activities Of the Cox-2 Enzymementioning

confidence: 99%

COX-2 inhibitors from the leaves of Pellacalyx saccardianus Scortech (Rhizophoraceae)

Abed

Sirat

Zulkifli

2015

Phytochemistry Letters

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Section: Inhibitory Activities Of the Cox-2 Enzymementioning

confidence: 99%

COX-2 inhibitors from the leaves of Pellacalyx saccardianus Scortech (Rhizophoraceae)

Abed

Sirat

Zulkifli

2015

Phytochemistry Letters

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“…The uorine atoms of the disorderd CF 3 -group were located on a di erence Fourier map and re ned freely. chemistry as pharmacophores or auxophores possessing diverse pharmacological activities, including antibacterial [1][2][3][4][5], anticancer [6][7][8][9][10], antiviral [11][12][13], antihypertensive [14,15], anti-in ammatory [16,17] and antioxidant [18] activities. In addition, some 1,3,4-oxadiazoles are currently used as safe herbicides for crop protection [19][20][21].…”

Section: Methodsmentioning

confidence: 99%

Crystal structure of 2-[3,5-bis(trifluoromethyl)benzylsulfanyl]-5-(5-bromothiophen-2-yl)-1,3,4-oxadiazole, C₁₅H₇BrF₆N₂OS₂

Al-Omary

Alanazi

Ghabbour

et al. 2016

Zeitschrift Für Kristallographie - New Crystal Structures

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C15H7BrF 6 N 2 OS 2 , monoclinic, P21/c (no. 14), a = 18.8292(14) Å, b = 11.4568(9) Å, c = 8.3400 (6) CCDC no.: 1481834The crystal structure is shown in the gure. Tables 1 and 2 contain details on crystal structure and measurement conditions and a list of the atoms including atomic coordinates and displacement parameters. Source of material3,5-Bis(tri uoromethyl)benzyl bromide (614 mg, 2.0 mmol) and anhydrous potassium carbonate (276 mg, 2.0 mmol) were added to a solution of 5-(5-bromothiophen-2-yl)-1,3,4-oxadiazole-2-thiol (526 mg, 2.0 mmol), in N,Ndimethylformamide (5 mL), and the mixture was stirred 87, 121.92, 124.76, 125.75, 130.52, 130.87, 131.51, 132.60, 141.38 Experimental detailsH atoms were placed in calculated positions and were included in the re nement in the riding model approximation. The uorine atoms of the disorderd CF 3 -group were located on a di erence Fourier map and re ned freely. Discussion1,3,4-Oxadiazole derivatives were early identi ed as a structural motif of particular interest in medicinal chemistry, material sciences and agrochemistry. Some 1,3,4-oxadiazoles have occupied a unique situation in the eld of medicinal

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“…Among the compounds tested, 9g was found to be the most potent inhibitor of COX-2 with IC 50 of 0.31 μM showing promising degree of anti-inflammatory activity in the carrageenan-induced rat paw edema model with ED 50 of 74.3 mg/kg [13] (Figure 13).…”

Section: Anti-inflammatorymentioning

confidence: 99%

Latest Update on Pharmacological Activities of 1,3,4-Oxadiazole Derivatives

Kumar¹,

Kumar²

2016

J Cell Sci Ther

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Heterocyclic compounds have been an interesting area for the study of synthesis and biological activity of novel oxadiazole derivatives for a long time. Heterocyclic compounds possess diverse biological properties that have led to intense study and research of these compounds. One of these compounds 1,3,4-Oxadiazole is a versatile heterocyclic nucleus is a novel molecule which attract the medicinal chemist to search a new therapeutic molecule. 1,3,4-oxadizole exhibited a wide range of biological activities which includes antimicrobial activity, anti-tubercular, anticonvulsant, antidiabetic, anti-allergic, enzyme inhibitors, anti-HIV activity, antipyretic activity, Immunosuppressive activity, Spasmolytic Activity, antioxidant activity, Anti-Alzheimer's activity cardiovascular acivity, anti-inflammatory, anti-tumor activity, insecticidal activity, CGRP receptor antagonists, anti-anthelmintic activities. Results of various derivatives of different oxadiazole and their substitutions with diverse biological activities are reviewed in present article.

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Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity

Cited by 92 publications

References 36 publications

COX-2 inhibitors from the leaves of Pellacalyx saccardianus Scortech (Rhizophoraceae)

COX-2 inhibitors from the leaves of Pellacalyx saccardianus Scortech (Rhizophoraceae)

Crystal structure of 2-[3,5-bis(trifluoromethyl)benzylsulfanyl]-5-(5-bromothiophen-2-yl)-1,3,4-oxadiazole, C₁₅H₇BrF₆N₂OS₂

Latest Update on Pharmacological Activities of 1,3,4-Oxadiazole Derivatives

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Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity

Cited by 92 publications

References 36 publications

COX-2 inhibitors from the leaves of Pellacalyx saccardianus Scortech (Rhizophoraceae)

COX-2 inhibitors from the leaves of Pellacalyx saccardianus Scortech (Rhizophoraceae)

Crystal structure of 2-[3,5-bis(trifluoromethyl)benzylsulfanyl]-5-(5-bromothiophen-2-yl)-1,3,4-oxadiazole, C15H7BrF6N2OS2

Latest Update on Pharmacological Activities of 1,3,4-Oxadiazole Derivatives

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Crystal structure of 2-[3,5-bis(trifluoromethyl)benzylsulfanyl]-5-(5-bromothiophen-2-yl)-1,3,4-oxadiazole, C₁₅H₇BrF₆N₂OS₂