- Synthesis, anti-inflammatory and analgesic activities of arylidene-2-(3-chloroanilino)nicotinic acid hydrazides
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A new series of 2-(3-chloroanilino)nicotinic acid hydrazides 12a-p were synthesized and evaluated for their anti-inflammatory and analgesic activities. Most of the compounds have shown anti-inflammatory activity with a moderate-to-excellent activity range. Among them, 3-chloro 12d and 4-methoxyphenyl derivatives 12i exhibited the most potent anti-inflammatory activity relative to niflumic acid as the reference drug (95, 87, and 81 % reductions in inflammation, respectively). The compounds with the highest anti-inflammatory activity were subjected to analgesic assay and showed moderate-to-excellent analgesic activities. The 2,4-dimethoxyphenyl derivative (12j) exhibited the highest analgesic activity relative to niflumic acid (99.6 and 68 % activity, respectively).
- Navidpour, Latifeh,Shafaroodi, Hamed,Saeedi-Motahar, Ghazaleh,Shafiee, Abbas
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p. 2793 - 2802
(2014/05/06)
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- Synthesis of 2-(arylamino)nicotinic acids in high-temperature water
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In hydrothermal reactions at 150-180 °C, 2-(arylamino)nicotinic acids were synthesized by amination of 2-chloronicotinic acid with aromatic amine derivatives, with potassium carbonate as base. The procedure is efficient, environmentally friendly, and practical, with moderate to excellent yields (up to 98%). Springer Science+Business Media B.V. 2012.
- Li, Zhenghua,Xiao, Shangyou,Liang, Ronghui,Xia, Zhining
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p. 1691 - 1697
(2012/10/29)
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- Catalyst-free amination of 2-chloronicotinic acid in water under microwave irradiation
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A simple, efficient and environmental friendly method for the synthesis of 2-arylaminonicotinic acids derivatives by reacting 2-chloronicotinic acid with anilines with potassium carbonate as the base and water as the media under microwave irradiation is described. The synthesis of 2-arylaminonicotinic acids is important because they are nonsteroidal anti-inflammatory drugs.
- Li, Zheng-Hua,Xia, Zhi-Ning,Chen, Gang
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experimental part
p. 709 - 711
(2012/03/09)
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- The chemical reactivity of a known anti-psoriasis drug. Part 1: Further insights into the products resulting from oxidative cleavage
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The oxidative cleavage of the known anti-psoriasis drug 1 to give 2 has been reported previously. Due to the importance of accessing medium-sized ring containing systems via oxidative cleavage, this reaction has been revisited revealing additional informa
- Jones, Alan M.,Lorion, Magali M.,Lebl, Tomas,Slawin, Alexandra M.Z.,Philp, Douglas,Westwood, Nicholas J.
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experimental part
p. 9667 - 9674
(2011/02/25)
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- Activation and inhibition of kidney CLC-K chloride channels by fenamates
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CLC-K Cl- channels are selectively expressed in kidney and ear, where they are pivotal for salt homeostasis, and loss-offunction mutations of CLC-Kb produce Bartter's syndrome type III. The only ligand known for CLC-K channels is a derivative o
- Liantonio, Antonella,Picollo, Alessandra,Babini, Elena,Carbonara, Giuseppe,Fracchiolla, Giuseppe,Loiodice, Fulvio,Tortorella, Vincenzo,Pusch, Michael,Camerino, Diana Conte
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p. 165 - 173
(2007/10/03)
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- Substituted 1,3-Dihydro-2H-pyrrolopyridin-2-ones as Potential Antiinflammatory Agents
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A series of analogues based on the 1,3-dihydro-2H-pyrrolopyridin-2-one ring system have been synthesized and shown to possess oral antiinflammatory activity in both the reverse passive Arthus reaction (RPAR) pleural cavity assay in rats and in the adjuvant-induced arthritic rat model (AAR).Several members of this series additionally exhibit an inhibitory effect on the in vivo production of prostaglandin- and leukotriene-derived products or arachidonic acid metabolism although these compounds exhibit no significant inhibitory activity against the cyclooxygenase and 5-lipoxygenase enzymes in vitro.Structure-activity relationships in this series are discussed.
- Ting, Pauline C.,Kaminski, James J.,Sherlock, Margaret H.,Tom, Wing C.,Lee, Joe F.,et al.
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p. 2697 - 2706
(2007/10/02)
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- Antiallergy Agents. 1. Substituted 1,8-Naphthyridin-2(1H)-ones as Inhibitors of SRS-A Release
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A novel class of antiallergy agents, the substituted 1,8-naphthyridin-2(1H)-ones, is described.The present compounds are orally active, potent inhibitors of allergic and nonallergic bronchospasm in animal models.Structure-activity studies of the lead compound in this sereis, 1-phenyl-3-n-butyl-4-hydroxynaphthyridin-2(1H)-one (11), identified three compounds of interest, 1-phenyl-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (12), 1-(3'-chlorophenyl)-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (87), and 1-(3'-methoxyphenyl)-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (89).The mechanism of antiallergy activity may involve inhibition of the release of the sulfidopeptide leukotrienes. 1-Phenyl-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one, Sch 33303 (12), was selected for preclinical development as an antiallergy agent.
- Sherlock, Margaret H.,Kaminski, James J.,Tom, Wing C.,Lee, Joe F.,Wong, Shing-Chun,et al.
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p. 2108 - 2121
(2007/10/02)
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