Binding of sulfonylurea derivatives to bovine serum albumin: part II. The relationship of binding to albumin, chemical structure, and hypoglycemic activity of sulfonamide derivatives of 2-pyrazoline-1-carboxamide.
The relationship of binding to protein and hypoglycemic activity of 11 sulfonamide derivatives of 2-pyrazoline-1-carboxamide was tested. It has been shown that the hypoglycemic effect of the most potent compound of the series, SPC-703, is related to the unbound, but not to the total concentration of the drug in the rat serum. Binding to albumin increased with the increase of hydrophobic properties of the compounds investigated. The increased affinity to albumin may be responsible for low hypoglycemic activity of some of the compounds tested.
D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D002417:Cattle; D007004:Hypoglycemic Agents / Q000097:blood*; D011485:Protein Binding; D011720:Pyrazoles / Q000097:blood* / Q000494:pharmacology; D051381:Rats; D012710:Serum Albumin, Bovine / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000097:blood* / Q000494:pharmacology; D013453:Sulfonylurea Compounds / Q000378:metabolism*; D013997:Time Factors
D001798:Blood Proteins; D007004:Hypoglycemic Agents; D011720:Pyrazoles; D013449:Sulfonamides; D013453:Sulfonylurea Compounds; D012710:Serum Albumin, Bovine