piperidine/iekaisums

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ReN-1869 [(R)-1-(3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-3-piperidine carboxylic acid], a novel histamine H1 receptor antagonist, produces potent and selective antinociceptive effects on dorsal horn neurons after inflammation and neuropathy.

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Ielogoties Reģistrēties

We characterized the effect of a novel selective histamine H1 receptor antagonist, (R)-1-(3-(10,11-dihydro-5H-dibenzo [a,d] cyclohepten-5-ylidene)-1-propyl)-3-piperidine carboxylic acid (ReN-1869), on the responses of dorsal horn neurons in anesthetized rats after carrageenan induced-inflammation

Evaluation of anti-inflammatory and antibacterial potential of newly synthesized 4-(2-Keto-1-benzimidazollinyl) derivatives of piperidine.

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Ielogoties Reģistrēties

Benzimidazole and its derivatives found variety of biological activities, for the searching of its potent anti-inflammatory analogues, we synthesized four novel 4-(2-keto-1-benzimidazollinyl) piperidine derivatives (Q1 to Q4) by refluxing piperidine with substituted imidazole and subjected to

Benzophenone-N-ethyl piperidine ether analogues--synthesis and efficacy as anti-inflammatory agent.

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Ielogoties Reģistrēties

A sequence of substituted benzophenone-N-ethyl piperidine ether analogues has been synthesized and evaluated as orally active anti-inflammatory agents with reduced side effects. The anti-inflammatory and ulcerogenic activities of the compounds were compared with naproxen, indomethacin, and

Analgesic and anti-inflammatory properties of 4-propionyl-4-(4-chlorophenyl)-1-(3-dimethylaminopropyl)-piperidine dihydrochloride.

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Ielogoties Reģistrēties

4-propionyl-4-(4-chlorophenyl)-1-(3-dimethylaminopropyl)-piperidine dihydro-chloride (S8) showed in the hot plate test a marked analgesic activity with a better therapeutic index than that of pethidine. S8 possesses also anti-inflammatory (in short and long-term tests in vivo) as well as spasmolytic

N-Acyl-N-phenyl ureas of piperidine and substituted piperidines endowed with anti-inflammatory and anti-proliferative activities.

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Ielogoties Reģistrēties

Six series of N-acyl-N-phenyl ureas 1-6 of piperidine (1), and 2-ethyl- (2), 3-methyl- (3), 4-methyl- (4), 4-phenyl- (5), cis-2,6-dimethyl- (6) piperidine were synthesised and evaluated for their anti-inflammatory, anaesthetic, anti-pyretic properties. Some derivatives of series 1 and 5 were also

Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.

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Ielogoties Reģistrēties

The structural optimization of the molecules making them to fit into the active site pocket of COX-2 occupying the same space as covered by the natural substrate arachidonic acid helped in the emergence of compound 10 as an efficacious anti-inflammatory agent. Selective for COX-2 over COX-1,

[Anti-inflammatory activity of 3-(N-piperidine)-1,1-diphenyl-1-propanol methansulfonate (HH 212)].

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Ielogoties Reģistrēties

Piperidines with motor depressor and anti-inflammatory properties.

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Ielogoties Reģistrēties

Synthesis and evaluation of anti-inflammatory activity of some thiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones and their Michael addition products.

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Ielogoties Reģistrēties

Thiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones (4-10) were obtained in a one step synthesis by heating 3-aryl-5-mercapto-1,2,4-triazoles (3a-d) with chloroacetic acid and appropriate aromatic aldehyde in acetic acid and acetic anhydride in the presence of anhydrous NaOAc. Michael type addition of cyclic

Pharmacologic studies on anti-inflammatory activity of di- and triketopiperidine derivatives.

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Ielogoties Reģistrēties

A number of derivatives of piperidine-2,4,6-trione and oxazine-2,4-dione with cyclohexyl and allyl substituents at their ring were evaluated pharmacologically. Piperidine-2,4,6-trione compounds, regardless of type of substituent, were readily absorbed from the site of their introduction and

ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation.

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Ielogoties Reģistrēties

The tricyclic compound (R)-1-(3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-3-piperidine carboxylic acid (ReN 1869) is a novel, selective histamine H(1) receptor antagonist. It is orally available, well tolerated, easily enters the central nervous system (CNS) but no adverse

Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives.

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Ielogoties Reģistrēties

We have explored a series of spirocyclic piperidine amide derivatives (5) as tryptase inhibitors. Thus, 4 (JNJ-27390467) was identified as a potent, selective tryptase inhibitor with oral efficacy in two animal models of airway inflammation (sheep and guinea pig asthma models). An X-ray co-crystal

Design and synthesis of novel xanthine derivatives as potent and selective A2B adenosine receptor antagonists for the treatment of chronic inflammatory airway diseases.

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Ielogoties Reģistrēties

Adenosine induces bronchial hyperresponsiveness and inflammation in asthmatics through activation of A2B adenosine receptor (A2BAdoR). Selective antagonists have been shown to attenuate airway reactivity and improve inflammatory conditions in pre-clinical studies. Hence, the identification of novel,

Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH).

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Ielogoties Reģistrēties

The synthesis and structure-activity relationships (SAR) of a series of benzothiophene piperazine and piperidine urea FAAH inhibitors is described. These compounds inhibit FAAH by covalently modifying the enzyme's active site serine nucleophile. Activity-based protein profiling (ABPP) revealed that

Attenuation of gastric mucosal inflammation induced by indomethacin through activation of the A2A adenosine receptor in rats.

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Ielogoties Reģistrēties

BACKGROUND Nonsteroidal anti-inflammatory drugs (NSAIDs) such as indomethacin induce gastric mucosal lesions in part by the activation of inflammatory cells and the production of proinflammatory cytokines. The activation of adenosine A(2A) receptors inhibits inflammation by increasing cyclic AMP in

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