Antipyretic activity of new compounds 4-(3-oxo-1,2-benzisothiazolin-2-yl)phenylalkanoic acids, their esters, amides and 1,1-dioxide derivatives.
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.
D000577:Amides; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001646:Bile / Q000378:metabolism; D001831:Body Temperature / Q000187:drug effects; D002264:Carboxylic Acids / Q000494:pharmacology*; D002756:Cholagogues and Choleretics; D004952:Esters; D005260:Female; D005753:Gastric Mucosa / Q000187:drug effects; D007928:Lethal Dose 50; D011749:Pyrogens / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000139:chemically induced; D013844:Thiazoles / Q000494:pharmacology*
D000577:Amides; D000894:Anti-Inflammatory Agents, Non-Steroidal; D002264:Carboxylic Acids; D002756:Cholagogues and Choleretics; D004952:Esters; D011749:Pyrogens; D013844:Thiazoles