The synthesis and in vitro and in vivo stability of 5-fluorouracil prodrugs which possess serum albumin binding potency.
For a new drug delivery system of 5-fluorouracil, we prepared prodrugs possessing certain desired properties. The prodrugs, 1-(N-4-chlorophenyl-N-methylcarbamoyl)-5-fluorouracil and 1-(N-2,4-dichlorophenyl-N-methylcarbamoyl)-5-fluorouracil, contain high serum albumin binding potency and a comparably long half life in the bloodstream in vivo to Tegafur. These two prodrugs are expected to be retained in the bloodstream as a polymeric complex with albumin and to circulate in the body for a long time, like a polymeric prodrug.
Suda
Y
Y
Department of Chemistry, Faculty of Science, Osaka University, Japan.
Shimidzu
K
K
Sumi
M
M
Oku
N
N
Kusumoto
S
S
Nadai
T
T
Yamashita
S
S
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D004355:Drug Stability; D005472:Fluorouracil / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism; D006207:Half-Life; D006868:Hydrolysis; D066298:In Vitro Techniques; D011355:Prodrugs / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D011485:Protein Binding; D051381:Rats; D012709:Serum Albumin / Q000378:metabolism*; D005641:Tegafur / Q000097:blood
D011355:Prodrugs; D012709:Serum Albumin; D005641:Tegafur; D005472:Fluorouracil