New carriers for representative peptides and peptide drugs.
3,5-Disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivatives; 4a-g were prepared and found to be a promising prodrug approach for peptide drugs. The pH profile for their degradation in aqueous buffer solutions was determined using HPLC technique and accounted for, in terms of specific base-catalyzed reactions. All of the compounds however, showed high acid-stability. Enzymatic (human serum) hydrolysis of the different derivatives offered an advantageous range of t1/2's, the property that permits controlling onset and duration of actions of drugs.
Aboul-Fadl
T
T
Faculty of Pharmacy, University of Assiut, Egypt.
El Shorbagi
A N
AN
D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D006801:Humans; D007700:Kinetics; D010455:Peptides / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011355:Prodrugs / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D013829:Thiadiazines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D013871:Thiones / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics
D004337:Drug Carriers; D010455:Peptides; D011355:Prodrugs; D013829:Thiadiazines; D013871:Thiones