Author/Authors :
Elfatih Elzein، نويسنده , , Rao Kalla، نويسنده , , Xiaofen Li، نويسنده , , Thao Perry، نويسنده , , Tim Marquart، نويسنده , , Mark Micklatcher، نويسنده , , Yuan Li، نويسنده , , Yuzhi Wu، نويسنده , , Dewan Zeng، نويسنده , , Jeff Zablocki، نويسنده ,
Abstract :
A series of new selective, high affinity A1-AdoR agonists is reported. Compound 23 that incorporated a carboxylic acid functionality in the 4-position of the pyrazole ring displayed KiL value of 1 nM for the A1-AdoR and >5000-fold selectivity over the A3 and A2A-AdoRs. In addition, compound 19 that incorporated a carboxamide functionality in the 4-position of the pyrazole ring displayed subnanomolar affinity for the A1-AdoR (KiL = 0.6 nM) and >600-fold selectivity over the A3 and A2A-AdoRs.
