Antipyretic activity of new compounds 4-(3-oxo-1,2-benzisothiazolin-2-yl)phenylalkanoic acids, their esters, amides and 1,1-dioxide derivatives.

Abstract

Antipyretic activity of new compounds, 4-(3-oxo-1,2-benzisothiazolin-2-yl)phenylalkanoic acids, their esters, amides and 1,1-dioxide derivatives has been studied. The acid compound of the benzoic series (I:a), tested at graded doses, exerted a noticeable antipyretic action; it had two times the "potency" of benzisothiazolone but an almost equal "efficacy". Its "potency" however was not proportional to the development of gastric lesions and to the acute toxicity. A decreased pharmacological activity has been observed in phenylalkanoic acids in the following order: R = COOH greater than CH2COOCH greater than CH(CH3)COOH greater than CH(C2H5)COOH, probably due to their increasing lipophilic character. By contrast among 1,1-dioxide derivatives the most effective in preventing pyrogen-induced fever was the ethyl ester (V:c) of benzoic series which appeared to be as active as paracetamol. The interest arising from these observations is here after discussed.

• Authors: E Barocelli, G Morini, C Silva, F Bordi, P V Plazzi, M Impicciatore
• Journal: Pharmacological research communications (Pharmacol Res Commun) Vol. 18 Issue 2 Pg. 171-85 (Feb 1986) ISSN: 0031-6989 [Print] United States
• PMID: 3486426 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Amides
• Anti-Inflammatory Agents, Non-Steroidal
• Carboxylic Acids
• Cholagogues and Choleretics
• Esters
• Pyrogens
• Thiazoles

Topics

• Amides
• Animals
• Anti-Inflammatory Agents, Non-Steroidal
• Bile (metabolism)
• Body Temperature (drug effects)
• Carboxylic Acids (pharmacology)
• Cholagogues and Choleretics
• Esters
• Female
• Gastric Mucosa (drug effects)
• Lethal Dose 50
• Pyrogens (pharmacology)
• Rats
• Rats, Inbred Strains
• Stomach Ulcer (chemically induced)
• Thiazoles (pharmacology)