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.
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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)
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Chemical References |
- Amides
- Anti-Inflammatory Agents, Non-Steroidal
- Carboxylic Acids
- Cholagogues and Choleretics
- Esters
- Pyrogens
- Thiazoles
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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)
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