Pharmacological studies of the two new hypoglycaemic compounds 4-(3-methyl-5-oxo-2-pyrazolin-1-yl)benzoic acid and 1-(mesitylen-2-sulfonyl)-1H-1,2,4-triazole.
New compounds showing hypoglycaemic activity have been designed through a computer-aided method based on QSAR (quantitative structure activity 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-pyrazolin-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 mechanism based on the response to the oral glucose overcharge, decreasing the glycemia to lower levels as compared with tolbutamide, which is used as a standard drug, and reaching normal glycaemia at a similar time.
Antón-Fos
G M
GM
Department of Chemistry and Physics, Pharmacy Faculty, University of Valencia, Spain.
García-Doménech
R
R
Pérez-Giménez
F
F
Peris-Ribera
J E
JE
García-March
F J
FJ
Salabert-Salvador
M T
MT
D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D015195:Drug Design; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D008297:Male; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000494:pharmacology*
D001786:Blood Glucose; D007004:Hypoglycemic Agents; D011720:Pyrazoles; D014230:Triazoles; C089552:1-(mesitylen-2-sulfonyl)-1H-1,2,4-triazole; C089551:4-(3-methyl-5-oxo-2-pyrazolin-1-yl)benzoic acid