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Страна 1 од 158 резултати
Characterization of N-(adamantan-1-ylmethyl)-5-[(3R-amino-pyrrolidin-1-yl)methyl]-2-chloro-benzamide, a P2X7 antagonist in animal models of pain and inflammation.
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Recent evidence suggests that the P2X(7) receptor may play a role in the pathophysiology of preclinical models of pain and inflammation. Therefore, pharmacological agents that target this receptor may potentially have clinical utility as anti-inflammatory and analgesic therapy. We investigated and
Synthesis, biological evaluation and docking study of N-(2-(3,4,5-trimethoxybenzyl)benzoxazole-5-yl) benzamide derivatives as selective COX-2 inhibitor and anti-inflammatory agents.
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A series of N-(2-(3,4,5-trimethoxybenzyl)-benzoxazole-5-yl)benzamide derivatives (3a-3n) was synthesized and evaluated for its in vitro inhibitory activity against COX-1 and COX-2. The compounds with considerable in vitro activity (IC50 < 1 µM), were evaluated in vivo for their anti-inflammatory and
Biochemical, cellular, and anti-inflammatory properties of a potent, selective, orally bioavailable benzamide inhibitor of Rho kinase activity.
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Rho kinase, is the most widely studied downstream effector of the small Rho GTPase RhoA. Two Rho kinase isoforms have been described and are frequently referred to in the literature as ROCK1 and ROCK2. The RhoA-Rho kinase pathway has been implicated in the recruitment of cellular infiltrates to
1,4-Dihydroquinazolin-3(2H)-yl benzamide derivatives as anti-inflammatory and analgesic agents with an improved gastric profile: Design, synthesis, COX-1/2 inhibitory activity and molecular docking study.
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The design and synthesis of a new series of 1,4-dihydroquinazolin-3(2H)-yl benzamide derivatives (4a-o) as anti-inflammatory and analgesic agents and COX-1/2 inhibitors are reported. The target compounds (4a-o) were synthesized using a two-step scheme, and their chemical structures were confirmed
Synthesis of substituted benzamides as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 but do not cause gastric damage.
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Parsalmide (5-amino-N-butyl-2-(2-propynyloxy) benzamide) (5a), is a non-steroidal anti-inflammatory drug (NSAID), commercialised in Italy until 1985 with the brand name of Synovial(R), that has been widely used to treat arthritic patient. In addition, it was shown to spare gastric mucosa. Here we
JAK2-targeted anti-inflammatory effect of a resveratrol derivative 2,4-dihydroxy-N-(4-hydroxyphenyl)benzamide.
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Chemical derivatization of resveratrol has been widely conducted in an effort to overcome its chemical instability and therapeutic potential. In the present study, we examined the anti-inflammatory effects of resveratrol derivatives containing an amide functionality using in vitro macrophage models
Synthesis and evaluation of anti-inflammatory and analgesic activities of a novel series of substituted-N-(4-methyl-2-oxo-2H-chromen-7-yl) benzamides.
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A novel series of coumarinyl amides (IVa-l) have been synthesized by reacting 7-amino-4-methylcoumarin (III) with various substituted aromatic acid chlorides. IR, 1H NMR, 13C NMR and HRMS spectral data characterized the structure of the synthesized compounds. The title compounds were screened for in
Involvement of alpha2-adrenergic mechanisms in experimental analgesic and anti-inflammatory activities of a benzamide derivative.
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Several non-steroidal anti-inflammatory drugs of the N-pyridinyl-benzamide series that produce experimental peripheral and central anti-inflammatory effects possess a dopaminomimetic component and inhibit eicosanoid synthesis without acting directly on the enzymes classically involved in this
[Effects of an anti-inflammatory agent of benzamide structure, dexamethasone and indomethacin on experimental cerebral edema induced by phospholipase 2 in rats].
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Only a few molecules show any efficacy against brain edema. Different methods such as brain copper-wire implantation or arachidonic acid injection are used in the research of active drugs. A new model, involving injection of phospholipase A2, is described. The effect of an anti-inflammatory
Newly discovered anti-inflammatory properties of the benzamides and nicotinamides.
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Our laboratory has concentrated on the possible regulation the benzamides and nicotinamides may have on the processes of DNA repair and apoptosis. Recent reports have suggested that both apoptosis and inflammation are regulated by the transcription factor NF-kappaB. We have initiated studies
Rational Design and Synthesis of Benzamides as Non-ulcerogenic Anti-inflammatory Agents.
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In an attempt to find a new class of anti-inflammatory agents, a series of novel benzamides 3 (ab1-ab16) was synthesized by utilizing some arylideneoxazolones 2(az1-az4) having 2-acetyloxyphenyl substitution on their second position. IR, 1H-NMR, 13C NMR and HRMS, confirmed the structures of these
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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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 < 1 μM) were evaluated in vivo for their anti-inflammatory
Biological evaluation and molecular docking studies of nitro benzamide derivatives with respect to in vitro anti-inflammatory activity.
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A series of nitro substituted benzamide derivatives were synthesized and evaluated for their potential anti-inflammatory activities in vitro. Firstly, all compounds (1-6) were screened for their inhibitory capacity on LPS induced nitric oxide (NO) production in RAW264.7 macrophages. Compounds 5 and
Synthesis of N-[4-(alkyl)cyclohexyl]-substituted benzamides with anti-inflammatory and analgesic activities.
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Two series of N-[4-(alkyl)cyclohexyl]-substituted benzamides, i.e. a series of N-[4-(tert-butyl)cyclohexyl]-substituted benzamides and a series of N-[4-(ethyl)cyclohexyl]-substituted benzamides, were synthesised and evaluated for their anti-inflammatory and analgesic potencies, and gastrointestinal
An anti-inflammatory benzamide derivative inhibits the protein kinase C (PKC)-dependent pathway of ERK2 phosphorylation in murine macrophages.
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We have previously described benzamide derivatives that inhibited tumor necrosis factor (TNF) production from activated macrophages (Mphi) probably by interacting with a protein kinase C (PKC)-dependent pathway. To investigate their mode of action further, we first tested their effect on isolated
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