Diuretic activity of Mannich base derivatives of ethacrynic acid and certain ethacrynic acid analogues.
Various Mannich base derivatives of selected phenoxyacetic acid type diuretics were synthesized and their diuretic potency was evaluated in dogs. It is concluded that the Mannich bases possess little, if any, diuretic activity of their own. Those Mannich bases that do possess diuretic activity undoubtedly do so as a consequence of an elimination reaction (a retro-Michael type reaction) which yields the corresponding pharmacologically active alpha,beta-unsaturated ketone.
D000818:Animals; D002712:Chlorides / Q000652:urine; D004232:Diuretics / Q000008:administration & dosage / Q000138:chemical synthesis*; D004285:Dogs; D004355:Drug Stability; D004976:Ethacrynic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D005919:Glomerular Filtration Rate / Q000187:drug effects; D007275:Injections, Intravenous; D008297:Male; D008352:Mannich Bases / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology; D011188:Potassium / Q000652:urine; D012964:Sodium / Q000652:urine
D002712:Chlorides; D004232:Diuretics; D008352:Mannich Bases; D012964:Sodium; D004976:Ethacrynic Acid; D011188:Potassium