Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors |
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Authors: | 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 |
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Affiliation: | Johnson & Johnson Pharmaceutical Research & Development L.L.C., 1000 Route 202, Raritan, NJ 08869, USA. zsui@prius.jnj.com |
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Abstract: | A series of N(2)-furoyl and N(2)pyrimidinyl beta-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. |
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