- Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction
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In an effort to minimize side effects associated with low selectivity against PDE isozymes, we have successfully identified a series of 6,7,8-substituted quinzaolines as potent inhibitors of PDE5 with high level of isozyme selectivity, especially against PDE6 and PDE11. PDE5 potency and isozyme selectivity of quinazolines were greatly improved with substitutions both at 6- and 8-position. The synthesis, structure-activity relationships and in vivo efficacy of this novel series of potent PDE5 inhibitors are described.
- Kim, Young Hoon,Choi, Hojin,Lee, Jaekwang,Hwang, In-Chang,Moon, Seung Kee,Kim, Soo Jin,Lee, Hong Woo,Im, Dai Sig,Lee, Sung Sook,Ahn, Soon Kil,Kim, Sang Woong,Han, Cheol Kyu,Yoon, Jeong Hyeok,Lee, Kyung Joo,Choi, Nam Song
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scheme or table
p. 6279 - 6282
(2009/07/18)
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- QUINAZOLINE DERIVATIVE AS PHOSPHODIESTERASE INHIBITOR AND A PROCESS FOR PREPARING THE SAME
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The present invention relates to a quinazoline derivative, a preparation method thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, a hydrate thereof, a pharmaceutical composition comprising the same and use thereof as a therapeutic agent. The present inveniont relates to a quinazoline derivative exhibiting inhibitory activity against C
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Page/Page column 23; 28-29
(2010/11/30)
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