Synthesis, Anti‐Inflammatory Activity, and COX‐1/2 Inhibition Profile of Some Novel Non‐Acidic Polysubstituted Pyrazoles and Pyrano[2,3‐c]pyrazoles
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DOI: 10.1002/ardp.201700025
Abstract: The synthesis and evaluation of the anti‐inflammatory activity of some structure hybrids comprising basically the 5‐hydroxy‐3‐methyl‐1‐phenyl‐4‐substituted‐1H‐pyrazole scaffold directly linked to a variety of heterocycles and functionalities, or annulated as pyrano[2,3‐c]pyrazoles, is described. According to the… read more here.
Keywords: anti inflammatory; cox inhibition; cox; activity ... See more keywords
Synthesis, molecular docking, and pharmacological evaluation of N‐(2‐(3,5‐dimethoxyphenyl)benzoxazole‐5‐yl)benzamide derivatives as selective COX‐2 inhibitors and anti‐inflammatory agents
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DOI: 10.1002/ardp.201800008
Abstract: A series of N‐(2‐(3,5‐dimethoxyphenyl)benzoxazole‐5‐yl)benzamide derivatives (3am) was synthesized and evaluated for their in vitro inhibitory activity against COX‐1 and COX‐2. The compounds with considerable in vitro activity (IC50 read more here.
Keywords: anti inflammatory; cox inhibitors; dimethoxyphenyl benzoxazole; cox ... See more keywords
Design, synthesis, and biological evaluation of new pyrazino[1,2‐a]benzimidazole derivatives as selective cyclooxygenase (COX‐2) inhibitors
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DOI: 10.1002/ardp.201800265
Abstract: A new class of pyrazino[1,2‐a]benzimidazole derivatives possessing the SO2Me pharmacophore at the para position of the C‐3 phenyl ring was designed, synthesized, and tested for their cyclooxygenase‐2 (COX‐2) inhibitory, anti‐cancer and anti‐platelet aggregation activities. In… read more here.
Keywords: pyrazino benzimidazole; cox; cyclooxygenase cox; benzimidazole derivatives ... See more keywords
Design and synthesis of pyrazole–pyrazoline hybrids as cancer‐associated selective COX‐2 inhibitors
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DOI: 10.1002/ardp.202000116
Abstract: In continuation of our previous work on cancer and inflammation, 15 novel pyrazole–pyrazoline hybrids (WSPP1–15) were synthesized and fully characterized. The formation of the pyrazoline ring was confirmed by the appearance of three doublets of… read more here.
Keywords: pyrazole pyrazoline; pyrazoline; pyrazoline hybrids; cox ... See more keywords
New pyrimidine/thiazole hybrids endowed with analgesic, anti-inflammatory, and lower cardiotoxic activities: Design, synthesis, and COX-2/sEH dual inhibition.
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DOI: 10.1002/ardp.202200024
Abstract: Some cyclooxygenase (COX)-2 selective medications were withdrawn from the market just a few years after their production due to cardiovascular side effects. In this study, a new series of pyrimidine/thiazole hybrids 7a-p was synthesized as… read more here.
Keywords: pyrimidine thiazole; cox; analgesic anti; anti inflammatory ... See more keywords
A new series of thiosemicarbazone‐based anti‐inflammatory agents exerting their action through cyclooxygenase inhibition
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DOI: 10.1002/ardp.202200136
Abstract: In an endeavor to identify potent anti‐inflammatory agents, new thiosemicarbazones (TSCs) incorporated into a diaryl ether framework (2a–2l) were prepared and screened for their in vitro inhibitory effects on cyclooxygenases (COXs). 4‐[4‐(Piperidin‐1‐ylsulfonyl)phenyl]‐1‐[4‐(4‐cyanophenoxy)benzylidene]thiosemicarbazide (2c) was the… read more here.
Keywords: series thiosemicarbazone; cox; inflammatory agents; anti inflammatory ... See more keywords
Discovery of novel pyrazole and pyrazolo[1,5‐a]pyrimidine derivatives as cyclooxygenase inhibitors (COX‐1 and COX‐2) using molecular modeling simulation
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DOI: 10.1002/ardp.202200395
Abstract: Searching for effective and selective anti‐inflammatory agents, our study involved designing and synthesizing new pyrazole and pyrazolo[1,5‐a]pyrimidine derivatives 4–11. The structures of the synthesized derivatives were confirmed using different spectroscopic techniques. Virtual screening was achieved… read more here.
Keywords: pyrazole pyrazolo; cox; pyrazolo pyrimidine; cox cox ... See more keywords
SC‐560 and mofezolac isosteres as new potent COX‐1 selective inhibitors with antiplatelet effect
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DOI: 10.1002/ardp.202200549
Abstract: Selective cyclooxygenase (COX)‐1 inhibitors can be employed as potential cardioprotective drugs. Moreover, COX‐1 plays a key role in inflammatory processes and its activity is associated with some types of cancer. In this work, we designed… read more here.
Keywords: new potent; cox; potent cox; mofezolac isosteres ... See more keywords
Simulating the slow to fast switch in cytochrome c oxidase catalysis by introducing a loop flip near the enzyme's cytochrome c (substrate) binding site
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DOI: 10.1002/bab.1526
Abstract: The mitochondrial enzyme cytochrome c oxidase catalyzes the reduction of molecular oxygen in the critical step of oxidative phosphorylation that links the oxidation of food consumed to ATP production in cells. The enzyme catalyzes the… read more here.
Keywords: cytochrome oxidase; cytochrome; cox; enzyme cytochrome ... See more keywords
Prostaglandin production by the microalga with heterologous expression of cyclooxygenase
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DOI: 10.1002/bit.27792
Abstract: Prostaglandins (PGs) are the physiologically active compounds synthesized from C20 polyunsaturated fatty acids (PUFAs) by cyclooxygenase (COX) and a series of PG synthases, and are utilized as pharmaceuticals. Currently, commercialized PGs are mainly produced by… read more here.
Keywords: production microalga; cyclooxygenase; prostaglandin production; cox ... See more keywords
Isoalantolactone inhibits IKKβ kinase activity to interrupt the NF‐κB/COX‐2‐mediated signaling cascade and induces apoptosis regulated by the mitochondrial translocation of cofilin in glioblastoma
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DOI: 10.1002/cam4.2013
Abstract: Isoalantolactone (IATL), a sesquiterpene lactone compound, possesses many pharmacological and biological activities, but its role in glioblastoma (GBM) treatment is still unknown. The aim of the current study was to investigate the antiglioma effects of… read more here.
Keywords: glioblastoma; isoalantolactone; cox; expression ... See more keywords