Novel Anti-Inflammatory Agents

Cullen, Ernest

doi:10.1002/jps.2600730503

Cited by 32 publications

(14 citation statements)

References 78 publications

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“…%~'J It is demonstrated in animal models that a variety of non-acidic NSAIDs are well tolerated by the gastric mucosa (Takesue et al 1976;Shen 1977;Gubler and Baggliolini 1978;Whittle et al 1980;Cullen 1984;Luzzani et al 1984). Thus, non-acidic NSAIDs with sufficient basic character will exist as an ionised species in the external milieu of the gastric parietal cell and a priori will not accumulate intracellularly (McCormack and Brune 1987).…”

Section: Introductionmentioning

confidence: 95%

The amphiprotic character of azapropazone and its relevance to the gastric mucosa

McCormack

Brune

1990

Arch Toxicol

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Since most non-steroidal anti-inflammatory drugs (NSAIDs) contain only one obvious ionisable group at physiological pH levels then they may be easily identified as having either acidic or basic character. Basic NSAIDs are simply non-acidic NSAIDs capable of accepting a proton within the physiological pH range. Within this range, however, a few NSAIDs contain two obvious ionisable groups, one acidic and the other basic. Such compounds should be described as amphiprotic, and include NSAIDs such as 4- and 5-amino substituted salicylic acids, niflumic acid, amfenac, WY 18251, and azapropazone. The aqueous ionisation equilibrium of such compounds is complex and is described by two macroscopic ionisation constants. Evidence has accumulated during the last decade to support the view that the pharmacokinetic behaviour of NSAIDs contributes not only decisively to their therapeutic effects but also to the type and incidence of their side-effects. A priori, using a physicochemical argument, certain amphiprotic NSAIDs should be better tolerated by the gastric mucosa than the classical acidic compound. Of those NSAIDs commercially available in the United Kingdom azapropazone remains the only one for which amphiprotic behaviour has been described. Following our examination of available data for azapropazone we conclude that the use of amphiprotic compounds represents a logical approach towards solving the problem of NSAID-induced gastric mucosal damage.

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Section: Introductionmentioning

confidence: 95%

The amphiprotic character of azapropazone and its relevance to the gastric mucosa

McCormack

Brune

1990

Arch Toxicol

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“…Previous phytochemical studies with A. excelsa have demonstrated the presence of quassinoids [5][6][7][8][9], alkaloids [10], terpenoids [11], and proteins [12]. A. excelsa extracts and some isolated compounds have demonstrated pharmacological properties such as significant antileukemic [13,14], antibacterial [15], antifungal [16], antimalarial [17], and antifertility activities [18]. While other species of the Simaroubaceae family have been investigated for their antiulcer efficacy [19], A. excelsa, which is used against gastrointestinal disturbances, has never actually been investigated for this property.…”

Section: Introductionmentioning

confidence: 99%

Gastroprotective and antisecretory effects of Ailanthus excelsa (Roxb)

et al. 2009

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Ailanthus excelsa (Roxb), an Egyptian medicinal species highly important for treating numerous diseases, was investigated against experimentally induced gastric ulcer in rodents. We evaluated the gastroprotective effect of four extracts (petroleum ether, diethyl ether, chloroform, and methanol) of A. excelsa bark by using the ethanol-induced gastric lesion model. The pretreatment of animals with methanolic, petroleum ether, and chloroformic extracts (100 mg/kg, oral (p.o.)) from A. excelsa significantly reduced gastric lesion induced by ulcerogenic agent (56, 47, and 70%, respectively) when compared with animals pretreated with vehicle. However, the diethyl ether pretreatment led to the least gastric lesion damage (83%), similar to the standard antiulcer drug, cimetidine, at the same dose (100 mg/kg, p.o.). The lower effective dose of diethyl ether extract, as well as cimetidine, given by intraduodenal route, significantly increased the pH values and reduced the acid output of gastric juice. Sterols, triterpenes,and quassinoids are present in the diethyl ether extract of A. excelsa stem bark, which presented the best gastroprotective action among the studied extracts. Our study confirmed the traditional indications of A. excelsa for the treatment of gastric ulcer.

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“…The currently available NSAIDs belong to different classes 19. Among the nonselective NSAIDs, we have indomethacin that is tenfold more active than COX‐1 while among selective COX‐2 inhibitors there are the pyrazolyl derivatives 20.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Pharmacological Evaluation of Some 4‐Oxo‐quinoline‐2‐carboxylic Acid Derivatives as Anti‐inflammatory and Analgesic Agents

Mazzoni¹,

Esposito²,

Diurno³

et al. 2010

Archiv der Pharmazie

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The synthesis and the pharmacological activity of a series of 1-aroyl derivatives of kynurenic acid methyl ester (4-oxo-quinolin-2-carboxy methyl (KYNA) esters), structurally related to NSAID indomethacin are described. The derivatives were screened in vivo for anti-inflammatory and analgesic activities. Most of the compounds exhibited good anti-inflammatory and analgesic activities. An automatic docking of the synthesized compounds was performed using X-ray structures of COX-1 and COX-2. Docking results are in good accordance with the experimental biological data.

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Novel Anti-Inflammatory Agents

Cited by 32 publications

References 78 publications

The amphiprotic character of azapropazone and its relevance to the gastric mucosa

The amphiprotic character of azapropazone and its relevance to the gastric mucosa

Gastroprotective and antisecretory effects of Ailanthus excelsa (Roxb)

Synthesis and Pharmacological Evaluation of Some 4‐Oxo‐quinoline‐2‐carboxylic Acid Derivatives as Anti‐inflammatory and Analgesic Agents

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