Synthesis and the antiperoxidase activity of seleno analogues of the antithyroid drug propylthiouracil.
The synthesis of 6-n-propyl-2-selenouracil (PSeU, Ib) and its methyl derivative (MSeU, Ic) are described. Replacement of the sulfur atom at C2 by selenium increased with antiperoxidase activity of these analogues five fold when compared to the clinically used antithyroid drug propylthiouracil (PTU). The structure-activity relationships of these agents are discussed.
Aboul-Enein
H Y
HY
Bioanalytical and Drug Development Laboratory, MBC-03 King Faisal Specialist Hospital and Research Centre, Riyadh, Kingdom of Saudi Arabia.
Awad
A A
AA
al-Andis
N M
NM
D000818:Animals; D010544:Peroxidases / Q000037:antagonists & inhibitors*; D011441:Propylthiouracil / Q000031:analogs & derivatives* / Q000494:pharmacology; D018036:Selenium Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013552:Swine; D013961:Thyroid Gland / Q000187:drug effects / Q000201:enzymology
D018036:Selenium Compounds; D011441:Propylthiouracil; D010544:Peroxidases