Source:http://linkedlifedata.com/resource/pubmed/id/15006407
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
|
pubmed:dateCreated |
2004-3-9
|
pubmed:abstractText |
In 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.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/3',5'-Cyclic-GMP Phosphodiesterases,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic Nucleotide...,
http://linkedlifedata.com/resource/pubmed/chemical/PDE5A protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphodiesterase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolines
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
0960-894X
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
22
|
pubmed:volume |
14
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1577-80
|
pubmed:dateRevised |
2007-11-15
|
pubmed:meshHeading |
pubmed-meshheading:15006407-3',5'-Cyclic-GMP Phosphodiesterases,
pubmed-meshheading:15006407-Cyclic Nucleotide Phosphodiesterases, Type 5,
pubmed-meshheading:15006407-Erectile Dysfunction,
pubmed-meshheading:15006407-Humans,
pubmed-meshheading:15006407-Male,
pubmed-meshheading:15006407-Phosphodiesterase Inhibitors,
pubmed-meshheading:15006407-Quinolines
|
pubmed:year |
2004
|
pubmed:articleTitle |
Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
|
pubmed:affiliation |
Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. ybi@lexpharma.com
|
pubmed:publicationType |
Journal Article
|