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pubmed-article:15006407pubmed:abstractTextIn a continuing effort to discover novel chemotypes as potent and selective PDE5 inhibitors for the treatment of male erectile dysfunction (ED), we have found that 4-benzylaminoquinoline derivatives are very potent and selective PDE5 inhibitors. Some compounds in this series had PDE5 IC(50)'s as low as 50 pM. While an electron withdrawing group at the C6-position of the quinoline substantially improved PDE5 potency, an ethyl group at the C8-position not only improved the PDE5 potency but also the isozyme selectivity. Substitutents at the C3-position can incorporate a variety of different groups. The synthesis and primary structure-activity relationship of this new series of potent PDE5 inhibitors are described.lld:pubmed
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pubmed-article:15006407pubmed:pagination1577-80lld:pubmed
pubmed-article:15006407pubmed:dateRevised2007-11-15lld:pubmed
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pubmed-article:15006407pubmed:year2004lld:pubmed
pubmed-article:15006407pubmed:articleTitleQuinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.lld:pubmed
pubmed-article:15006407pubmed:affiliationDepartment of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. ybi@lexpharma.comlld:pubmed
pubmed-article:15006407pubmed:publicationTypeJournal Articlelld:pubmed
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