Anti-inflammatory/anti-pyretic salicylic acid esters with low gastric ulcerogenic activity

Agents and Actions
K D Rainsford, M W Whitehouse

Abstract

The methyl and some other esters of acetylsalicylic and salicylic acids and their derivatives were found to have much lower gastric ulcerogenic activity (when assayed in the stress-sensitized rat) compared with their corresponding acids. There was little or no loss in therapeutic potencies of these salicylate esters as determined by assessment of anti-inflammatory activity (against the carrageenan-induced oedema) and antipyretic activity (against yeast-induced fever in rats. The methyl ester of acetylsalicylic acid (=AME) was almost devoid of gastric irritancy/ulcerogenicity (as observed with acetylsalicylic acid) when given orally to pigs for 10 days. AME had appreciable anti-inflammatory activity in the adjuvant-arthritis model and at high doses (200 mg/kg t.i.d.) was without the lethal effects seen with acetylsalicylic acid. Moreover, no toxic effects were seen after long-term administration of 100-1000 mg/kg/day AME for 3-4 months. The results provide further evidence for the hypothesis that the carboxylic acid moiety of salicylates is a major factor in the gastric ulcerogenic activity of these drugs. The methyl esters of these salicylates may be considered as models for the development of pro-drugs and in some cases may be...Continue Reading

References

Oct 1, 1975·Agents and Actions·K D Rainsford
Jul 1, 1976·The Journal of Pharmacy and Pharmacology·K D Rainsford, M W Whitehouse
Feb 1, 1978·The Journal of Pharmacy and Pharmacology·K D Rainsford
Dec 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·J A WalderI M Klotz
Jan 1, 1977·Agents and Actions. Supplements·M W Whitehouse, K D Rainsford
Jan 1, 1976·Australian and New Zealand Journal of Medicine·J R Leonards
Jan 1, 1976·Drugs·A R Cooke
Jan 1, 1980·Pharmacological Research Communications·K D Rainsford, M W Whitehouse
Nov 1, 1980·Agents and Actions·K D RainsfordK Brune

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Citations

Nov 1, 1980·Agents and Actions·K D RainsfordK Brune
Oct 12, 2001·Journal of Physiology, Paris·K D Rainsford
Aug 7, 2009·Natural Product Research·Saikat DewanjeeSubhash C Mandal
Jun 20, 2012·AAPS PharmSciTech·Pinaki GhoshShivajirao S Kadam
Jun 9, 2007·Alimentary Pharmacology & Therapeutics·I BjarnasonK D Rainsford
Apr 18, 2008·The Journal of Pharmacy and Pharmacology·Anil K PhilipKamla Pathak
Dec 12, 2012·Bioorganic & Medicinal Chemistry Letters·Suneela DhaneshwarGourav Meena
Dec 7, 2010·European Journal of Medicinal Chemistry·Peng-Cheng LvHai-Liang Zhu
Jun 14, 2003·Fundamental & Clinical Pharmacology·Brendan J R Whittle
Dec 4, 2008·Journal of Medicinal Chemistry·Louise M MoriartyJohn F Gilmer
Jul 9, 2021·Frontiers in Pharmacology·L McEvoyM Pirmohamed

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