PHARMACOLOGICAL STUDIES OF THE 2 NEW HYPOGLYCEMIC COMPOUNDS 4-(3-METHYL-5-OXO-2-PYRAZOLIN-1-YL)BENZOIC ACID AND 1-(MESITYLEN-2-SULFONYL)-1H-1,2,4-TRIAZOLE
Gm. Antonfos et al., PHARMACOLOGICAL STUDIES OF THE 2 NEW HYPOGLYCEMIC COMPOUNDS 4-(3-METHYL-5-OXO-2-PYRAZOLIN-1-YL)BENZOIC ACID AND 1-(MESITYLEN-2-SULFONYL)-1H-1,2,4-TRIAZOLE, Arzneimittel-Forschung, 44-2(7), 1994, pp. 821-826
New compounds showing hypoglycaemic activity have been designed hrough
a computer-aided method based on QSAR (quantitative structure activit
y relationship) and molecular connectivity. The pharmacological tests
carried out on the newly designed compounds demonstrated the existence
of notable activity for two of them, namely: 4-(3-methyl-5-oxo-2-pyra
zolin-1-yl) benzoic acid (CAS 60875-16-3) and 1-(mesitylen-2-sulfonyl)
-1H-1,2,4-triazole (CAS 54230-59-0). Both substances mainly follow a m
echanism based on the response to the oral glucose overcharge, decreas
ing the glycemia to lower levels as compared with tolbutamide, which i
s used as a standard drug, and reaching normal glycaemia at a similar
time.