Author/Authors :
Zhihua Sui، نويسنده , , Jihua Guan، نويسنده , , Mark J. Macielag، نويسنده , , Weiqin Jiang، نويسنده , , Yuhong Qiu، نويسنده , , Patricia Kraft، نويسنده , , Sheela Bhattacharjee، نويسنده , , T. Matthew John، نويسنده , , Elizabeth Craig، نويسنده , , Donna Haynes-Johnson، نويسنده , , Joanna Clancy، نويسنده ,
Abstract :
A series of N2-furoyl and N2pyrimidinyl β-carbolines was discovered to possess potent inhibitory activity against PDE5. During the synthesis we developed a tandem resin quenching protocol, which allowed us to synthesize large number of target compounds in a rapid fashion. Representative compounds exhibit superior selectivity to sildenafil versus other isozymes of PDEs, and demonstrated in vivo efficacy in increasing introcavernosal pressure in dogs.
