Author/Authors :
Moo Hong Lim، نويسنده , , Hea Ok Kim، نويسنده , , Hyung Ryong Moon، نويسنده , , Seung-Jin Lee، نويسنده , , Moon Woo Chun and، نويسنده , , Zhan-Guo Gao، نويسنده , , Neli Melman، نويسنده , , Kenneth A. Jacobson، نويسنده , , Joong Hyup Kim، نويسنده , , Lak Shin Jeong، نويسنده ,
Abstract :
Several 3′-fluoro analogues, 1a, 1b, and 1c of selective and potent adenosine A3receptor agonist, Cl-IB-MECA were synthesized from -xylose via highly regioselective opening of lyxo-epoxides, 8a and 8b with fluoride anion. Compared to the high binding affinity of Cl-IB-MECA to the A3 adenosine receptor, the corresponding 3′-fluoro derivative showed remarkably decreased binding affinity, indicating that 3′-hydroxyl group acts as hydrogen bonding acceptor, not hydrogen bonding donor like fluorine atom in binding to the A3 adenosine receptor.
