N-sugar derivs. of ortho- and meta-amino-benzoic acid - have hypoglycaemic, hypotensive, hypolipaemic, antiinflammatory, analgesic, antipyretic, and antitumour activity

摘要

Aminobenzoic acid derivs. of formula R1-NH-Ph-COOR2 are new. R1 is a gp. formed by removal of the 1-alpha or 1-beta hydroxy gp. from ribose, 2-desoxyribose- fructose, sorbase, fucose, maltose, saccharose, lactose, cellobiose, malto- triose, gluconolactone, N-methyl-glucuronic acid or acetylglucosamine; R1-NH to joined in the ortho or meta position w.r.t. -COOR2; R2 is H, Na, K, 1/2Mg, 1/2Ca, 1/3Al or 1-4C alkyl. Hypoglycemic, hypotensive, hypolipaemic, antiinflammatory, anagesic, antipyretic and antitumour cpds. which may be administered orally (0.1-500, pref. 1-250, mg/kg/day) or parenterally (0.01-200, pref. 0.1-100, mg/kg/day). Extensive pharmacological tests are described e.g. antitumour activity is demonstrated against sarcoma 180 tumour transplanted in mice. The cpds. have low toxicity (LD50 in mice of tested cpds. 4.1- 11.6 g/kg) and no antibacterial activity (do not disturb intestinal bacteria) and do not effect immunity.