Linked Life Data

12824033

Source:http://linkedlifedata.com/resource/pubmed/id/12824033

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
14
pubmed:dateCreated
2003-6-25
pubmed:abstractText
A new series of catechol hydrazines was synthesized and their structure-activity relationship (SAR) was analyzed for developing an effective phosphodiesterase 4 (PDE4) inhibitor as an anti-asthmatic drug candidate. Among the (E)-Analogues tested using in vitro assays, 5CC showed a strong PDE4 inhibitory activity and a significantly improved rolipram binding profile compared with rolipram, a prototype PDE4 inhibitor. Moreover, from in-vivo asthma model, we observed that (E)-Analogue 5CC had a good efficacy against guinea-pig respiratory tract inflammation and bronchoconstriction, along with a remarkably reduced emetic side effect, compared with rolipram. Conclusively, (E)-Analogue 5CC seems to be a promising candidate for the development of anti-asthmatic PDE4 inhibitors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0960-894X
pubmed:author
pubmed:issnType
Print
pubmed:day
21
pubmed:volume
13
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2355-8
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed-meshheading:12824033-3',5'-Cyclic-AMP Phosphodiesterases, pubmed-meshheading:12824033-Animals, pubmed-meshheading:12824033-Anti-Asthmatic Agents, pubmed-meshheading:12824033-Binding Sites, pubmed-meshheading:12824033-Brain, pubmed-meshheading:12824033-Bronchoalveolar Lavage Fluid, pubmed-meshheading:12824033-Bronchoconstriction, pubmed-meshheading:12824033-Cyclic Nucleotide Phosphodiesterases, Type 4, pubmed-meshheading:12824033-Ferrets, pubmed-meshheading:12824033-Guinea Pigs, pubmed-meshheading:12824033-Hydrazines, pubmed-meshheading:12824033-Inflammation, pubmed-meshheading:12824033-Models, Molecular, pubmed-meshheading:12824033-Muscle Relaxation, pubmed-meshheading:12824033-Phosphodiesterase Inhibitors, pubmed-meshheading:12824033-Rolipram, pubmed-meshheading:12824033-Structure-Activity Relationship, pubmed-meshheading:12824033-Trachea, pubmed-meshheading:12824033-Vomiting
pubmed:year
2003
pubmed:articleTitle
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
pubmed:affiliation
Pharmacology and Analytical Chemistry Research, 319 Hyundai I Valley, 223-12 Sandaewon-dong, Choongwon-gu, Sungnam-si, 462-120, Kyonggi-do, Republic of Korea. ekim@postech.ac.kr
pubmed:publicationType
Journal Article, In Vitro