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13 risultati
Pharmacology of the dual inhibitor of cyclooxygenase and 5-lipoxygenase 3-hydroxy-5-trifluoromethyl-N-(2-(2-thienyl)-2-phenyl-ethenyl)-benzo (b)thiophene-2-carboxamide.
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3-Hydroxy-5-trifluoromethyl-N-(2-(2-thienyl)-2-phenyl-ethenyl)- benzo (b) thiophene-2-carboxamide (L-652,343) is an inhibitor of cyclooxygenase and 5-lipoxygenase in vitro and inhibits the synthesis of the products of both these pathways in whole cells. L-652,343 is an inhibitor of the acute edema
Synthesis, in vivo anti-inflammatory, COX-1/COX-2 and 5-LOX inhibitory activities of new 2,3,4-trisubstituted thiophene derivatives
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New series of thiophene derivatives were synthesized and evaluated for their in vivo anti-inflammatory activity using carrageenan-induced paw edema model. The most active in vivo anti-inflammatory compounds 5b, 11b, 14c, 18c, 19c and 20d were further evaluated for their in vitro COX-1/COX-2 and
Design, synthesis, and pharmacological evaluation of some 2-[4-morpholino]-3-aryl-5-substituted thiophenes as novel anti-inflammatory agents: generation of a novel anti-inflammatory pharmacophore.
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Compounds incorporating a thiophene moiety, a pi excess five membered heterocycle, have attracted a great deal of research interest owing to the therapeutic utility of the template as useful drug molecular scaffolding. Recently we reported the anti-inflammatory activity profile exhibited by two
[Quantitative anti-inflammatory and analgesic structure-activity relationship of 2-amino-3-ethoxycarbonyl thiophene derivatives].
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Quantitative structure activity relationships of 2-amino-3-carboxylic acid ethyl ester thiophene derivatives are described. These compounds exhibit a weak anti-edema activity and a more significant analgesic activity relative to acetylsalicylic acid and oxyphenylbutazone. The application of
Tetra substituted thiophenes as anti-inflammatory agents: exploitation of analogue-based drug design.
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A series of 17 novel tetra substituted thiophenes was designed, synthesized, and screened for anti-inflammatory activity in carrageenin induced rat paw edema model, an acute in vivo model. The lead molecule selected was Tenidap, a dual COX/LOX inhibitor. Compounds I (43%), III (60%), IV (60%), and
Design, synthesis, and SAR studies of some 5-aliphatic oximino esters of thiophene as potential anti-inflammatory leads: comparative biological activity profile of aliphatic oximes vs aromatic oximes.
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A series of novel tetra substituted thiophenes were synthesized, characterized, and evaluated for their anti-inflammatory activity in carrageenin induced rat paw edema model-an acute in vivo model. Compounds V1, V3, V11, V12, V17, and V18 showed good anti-inflammatory activity, indicating the
Synthesis and biological evaluation of novel 2-(4-acetyl-3-methyl-5-(arylamino) thiophen-2-yl)-3-arylquinazolin-4(3H)-one derivatives as potential anti-inflammatory and antioxidant agents.
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BACKGROUND
A new series of 2-(4-acetyl-3-methyl-5-(arylamino) thiophen-2-yl)-3-arylquinazolin-4(3H)-one derivatives (11a-11j) were synthesized from acetyl acetone, phenyl isothiocyanate and 2-chloromethyl quinazolinone.
OBJECTIVE
Due to side effects of Non Steroidal anti-inflammatory drugs (NSAID),
[Structure-activity relationships of the thienothiazine derivatives with their antiinflammatory, analgesic and ulcerogenic effects and their inhibitory effects on PGE2 biosynthesis].
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A new series of thienothiazine derivatives were evaluated as a means of clarifying whether the changed chemical structure would have a different effect on carrageenin edema, scalded hyperalgesia and ulcerogenicity in rats and also have a different effect on PGE2 biosynthesis in vitro. The
Synthesis and pharmacochemical study of new Cu(II) complexes with thiophen-2-yl saturated and alpha,beta-unsaturated substituted carboxylic acids.
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Copper complexes with thiophen-2-yl saturated and alpha,beta-unsaturated carboxylic acids as ligands were prepared, characterized and pharmacochemically studied. The available evidence supports a dimeric structure for the complexes of the general formula [Cu2(L)4(MeOH)2] where L are the anions of
Novel drug designing approach for dual inhibitors as anti-inflammatory agents: implication of pyridine template.
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Compounds incorporating thiophene moiety, a pi excess five membered heterocycle, have attracted a great deal of research interest, owing to the therapeutic utility of the template as useful drug molecular scaffolding. We report the synthesis and pharmacological evaluation of thiophenes substituted
Effect of IKK-2 inhibitor on local Th1 and Th2 type inflammation.
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We studied the capacity of IKK-2 inhibitor ([5-(p-fluorophenyl)-2-ureido] thiophene-3-carboxamide) and non-steroidal anti-inflammatory drug voltaren to reduce the severity of local inflammation in Th1- and Th2-type immune response. The test substances (inhibitor in concentrations from 2×10(-13)to
Evaluation of anti-inflammatory and antioxidant activities of copper (II) Schiff mono-base and copper(II) Schiff base coordination compounds of dien with heterocyclic aldehydes and 2-amino-5-methyl-thiazole.
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Highly reactive radicals are implicated in many pathological conditions. The quest for radical scavengers or antioxidants, spans the previous decades. A new series of complexes of the type [Cu (dien) (2a-2tzn) Y(2)] and [Cu (dienXXY(2)) (2a-5mt)] and of the type [Cu (dptaS) Cl(2)] and [Cu (dptaS)
Characterization of cutaneous phototoxicity induced by topical alpha-terthienyl and ultraviolet A radiation.
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Alpha-terthienyl (alpha-T), a phototoxic thiophene compound isolated from marigolds (Tagetes species), affects cell membranes and does not appear to induce cytogenetic damage. This study was undertaken to investigate topical delivery of alpha-T and characterize its cutaneous phototoxicity in
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