Studio farmacologico di un nuovo coleretico derivato dall'acidoα-cicloesil butirrico

Inhibition of Human DHODH by 4‐Hydroxycoumarins, Fenamic Acids, and N‐(Alkylcarbonyl)anthranilic Acids Identified by Structure‐Guided Fragment Selection

“…4,5‐Dihydroxy‐3‐(4‐biphenyl)coumarin (23): The starting material 2‐biphenyl‐4‐ylmalonic acid diethyl ester was prepared according to a method already described 32. Compound 23 was synthesised from resorcinol and 2‐biphenyl‐4‐ylmalonic acid diethyl ester according to the procedure for compound 10 , to provide the product as an ivory‐white powder (170 mg, 5 %).…”

Basic Ethers of Guaiacol and Thymol with a Polyoxyethylenic Chain and Their Main Pharmacological Activities. New Antitussives

“…observing whether this w-as accompanied by hypotension and respiratory impairment, the acute LD50 in mice and albino rats,7 and the local anesthetic8 and analgesic activity.9•10 The occurence of central sedation was measured through variations in the spontaneous motility and in the performance of the grip test, and through the influence exerted by the compounds on the duration of the barbiturate narcosis. 11 The spasmolytic activity was tested on the isolated rat and guinea pig ileum against histamine, acetylcholine, BaCk, and nicotine contractions.12 Compound 15 was studied as antitussive also on unanesthetized rats and guinea pigs13•14 and further as an inhibitor of pentylenetetrazole seizures,11 for its effect on peristalsis,15 and on the bronchial and tracheal muscles in vivo and in vitro16•17; finally its influence upon the bronchial and tracheal secretion was examined. 18 In Table III only the compounds appreciably active as antitussives are recorded with the results concerning their antitussive, local anesthetic, analgetic, narcosis-enhancing, hypotensive, and respiratory-depressing activities and the data about their acute toxicity.…”