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Synthesis, antioxidant and antiinflammatory activity of novel aryla-cetic and aryl-hydroxamic acids.

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Four new aryl-acetic acids and the corresponding hydroxamic acids were synthesized. These compounds showed interesting interaction with the free radical 1,1-diphenyl-2-picryl-hydrazyl (DPPH), scavenging activity on .OH, inhibition of soybean lipoxygenase and a significant inhibition of carrageenin

Antioxidant and anti-inflammatory activity of aryl-acetic and hydroxamic acids as novel lipoxygenase inhibitors.

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Lipoxygenase plays an essential role in the biosynthesis of the leukotrienes. Leukotrienes, as LO metabolites of arachidonic acid (AA), have been implicated as mediators in the pathophysiology of inflammatory diseases, host defense reactions and to play important role in the propagation of the

Effects of suberoylanilide hydroxamic acid on rat cytochrome P450 enzyme activities.

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Vorinostat (suberoylanilide hydroxamic acid, SAHA) is the first approved histone deacetylase (HDAC) inhibitor for the treatment of cutaneous T-cell lymphoma after progressive disease following two systemic therapies. The rats were randomly divided into SAHA groups (low, medium and high dosage) and

Dibenzoxepinone hydroxylamines and hydroxamic acids: dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity.

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Hydroxylamine and hydroxamic acid derivatives of a known nonsteroidal antiinflammatory dibenzoxepine series display both cyclooxygenase (CO) and 5-lipoxygenase (5-LO) inhibitory properties. Many of these new dual CO/5-LO inhibitors also exhibit potent topical antiinflammatory activity in the

Discovery of potential anti-inflammatory drugs: diaryl-1,2,4-triazoles bearing N-hydroxyurea moiety as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.

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A series of hybrids from diaryl-1,2,4-triazole and hydroxamic acid or N-hydroxyurea were synthesized and evaluated as novel anti-inflammatory agents. The biological data showed that (i) all the compounds showed dual COX-2/5-LOX inhibitory activities in vitro, and 15e showed optimal inhibitory

Anti-inflammatory properties and inhibition of leukotriene C4 biosynthesis in vitro by flavonoid baicalein from Scutellaria baicalensis georgy roots.

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Anti-inflammatory activity of baicalein (5,6,7-trioxyflavone-7-O-beta-D-glucuronide) was greater in the chronic inflammation model (rat adjuvant arthritis, ED50 = 120.6 mg/kg) than observed in the rat carrageenan-induced paw edema, ED50 > or = 200.0 mg/kg. A comparative study of the 5-lipoxygenase

Valproic acid: an anticonvulsant drug with potent antinociceptive and anti-inflammatory properties.

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Valproic acid (VA) is a major antiepileptic drug, used for several therapeutic indications. It has a wide activity spectrum, reflecting on mechanisms of action that are not fully understood. The objectives of this work were to study the effects of VA on acute models of nociception and inflammation

Synthesis of 5-phenyl-1-(3-pyridyl)-1H-1,2,4-triazole-3-carboxylic acid derivatives of potential anti-inflammatory activity.

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A series of 5-phenyl-1-(3-pyridyl)-1H-1,2,4-triazole-3-carboxylic acid derivatives 4-10 were synthesized by rearrangement of 4-(3-pyridyl)-hydrazono-2-phenyl-2-oxazolin-5-one 3 in the presence of different nucleophiles to afford derivatives 4, 7, and 8, while hydroxamic acid derivative 6 was

Trioxsalen derivatives with lipoxygenase inhibitory activity.

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Trioxsalen (TRX) is a 4,5',8-trimethylated psoralen analog presenting interesting biological activities when irradiated with UVA light. A series of TRX derivatives, which where obtained by its chemical modification and incorporation of a variety of unsaturated functions at position 4' of the

New dextran derivatives. I. Nitrogen containing derivatives.

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Three new derivatives of dextran were obtained: 3-morpholine-2-hydroxypropyl ether of dextran (I), hydroxamic acid of carboxymethyl dextran (II), and oxime of ketodextran (III). All the three derivatives exhibited low toxicity at parenteral administration to laboratory animals. (I) and (II) showed

Structure-based design, synthesis, molecular docking, and biological activities of 2-(3-benzoylphenyl) propanoic acid derivatives as dual mechanism drugs.

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OBJECTIVE 2-(3-benzoyl phenyl)propanohydroxamic acid (2) and 2-{3-[(hydroxyimino)(phenyl)methyl]phenyl}propanoic acid (3) were synthesized from non-steroidal anti-inflammatory drug, ketoprofen as dual-mechanism drugs. METHODS Structures of the synthesized compounds were established by IR, (1)H NMR,

Epigenetic Modification Prevents Excessive Wound Healing and Scar Formation After Glaucoma Filtration Surgery.

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The purpose of this study was to determine the efficacy of suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor (HDACi), in prevention of excessive wound healing and scar formation in a rabbit model of glaucoma filtration surgery (GFS). A rabbit model of GFS was used. Rabbits that

Valproate administered after traumatic brain injury provides neuroprotection and improves cognitive function in rats.

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BACKGROUND Traumatic brain injury (TBI) initiates a complex series of neurochemical and signaling changes that lead to pathological events including neuronal hyperactivity, excessive glutamate release, inflammation, increased blood-brain barrier (BBB) permeability and cerebral edema, altered gene

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