Synthesis and biological activities of novel β-Carbolines as PDE5 inhibitors

…, TM John, E Craig, D Haynes-Johnson, J Clancy

文献索引：Sui, Zhihua; Guan, Jihua; Macielag, Mark J.; Jiang, Weiqin; Qiu, Yuhong; Kraft, Patricia; Bhattacharjee, Sheela; John, T. Matthew; Craig, Elizabeth; Haynes-Johnson, Donna; Clancy, Joanna Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 4 p. 761 - 765

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被引用次数: 16

摘要

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 ...