Preparation of a 3'-azido-3'-deoxythymidine (AZT) derivative, which is blood-brain barrier permeable.
The anti-AIDS drug AZT was covalently attached to the recently reported sorbitol-G8 transporter, and the conjugate was found to target mitochondria in HeLa cells and readily cross the blood-brain barrier (BBB) to gain access into the mouse brain, suggesting the potential of these molecular transporters as practical central nervous system (CNS) delivery vectors.
Im
Jungkyun
J
Department of Chemistry, Pohang University of Science and Technology, Pohang 790-784, Republic of Korea.
Kim
Wanil
W
Kim
Kyong-Tai
KT
Chung
Sung-Kee
SK
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D001812:Blood-Brain Barrier; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D018613:Microscopy, Confocal; D008928:Mitochondria / Q000187:drug effects*; D015394:Molecular Structure; D010539:Permeability; D015215:Zidovudine / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism
D019380:Anti-HIV Agents; D015215:Zidovudine