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Synthesis of Quaternary Ammonium Based New Analgesic, Anti- Inflammatory and Antipyretic Drugs

Thesis Info

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External Link

Author

Ullah, Nasir

Program

PhD

Institute

University of Peshawar

City

Peshawar

Province

KPK

Country

Pakistan

Thesis Completing Year

2012

Thesis Completion Status

Completed

Subject

Chemistry

Language

English

Link

http://prr.hec.gov.pk/jspui/handle/123456789/2109

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676727495330

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The carboxylic acid group (-COOH) present in most commercial NSAIDs is thought to be partly responsible for the gastric toxicity associated with the long-term administration of these compounds. The goal of the present research was to determine if new NSAID derivatives devoid of acidic moieties would retain the anti- inflammatory activity while exerting a lower degree of gastric toxicity compared to the corresponding parent NSAID. In this regard, we replaced the carboxylic acid group in aspirin, ibuprofen, flurbiprofen, and naproxen with a series of quaternary ammonium moieties, and the resulting water-soluble NSAID derivatives were tested for anti-inflammatory and ulcerogenic activity in vivo. Results of our investigation showed that replacement of quaternary ammonium moieties for the carboxylic acid group present in NSAIDs, yielded potent anti-inflammatory molecules without stomach ulceration when administered orally to rats. Among the new compounds, N- (2-hydroxyethyl)-2-(6-methoxynaphthalen-2-yl)propan-1-aminium chloride (a naproxen derivative) was the most potent anti-inflammatory agent (65.28% inhibition of inflammation at 6.4 mg/kg); however, unlike the reference compound naproxen (ulcer index = 108.7), N-(2-hydroxyethyl)-2-(6-methoxynaphthalen-2-yl)propan-1- aminium chloride did not produced gastric ulcers (Ulcer index = 0) when administered orally at equimolar doses (0.17mmol). These results suggest that the carboxylic acid group present in commercial 2-phenylpropionic acid NSAIDs is not an essential requirement for anti-inflammatory activity in vivo, and offers a new concept in drug design by using water-soluble ammonium moieties instead. Derivatives of salicylic acid were screened for analgesic, anti-inflammatory and antipyretic activities, and acute toxicity. The result of this study indicated that these compounds possess dose dependent statistically significant analgesic, anti- inflammatory and antipyretic properties, compared to aspirin, without causing gastric ulceration and acute toxicity.
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