rdf:type |
|
lifeskim:mentions |
umls-concept:C0002792,
umls-concept:C0003691,
umls-concept:C0003693,
umls-concept:C0005821,
umls-concept:C0020314,
umls-concept:C0021368,
umls-concept:C0027950,
umls-concept:C0033551,
umls-concept:C0205549,
umls-concept:C0243072,
umls-concept:C0443199,
umls-concept:C1280500,
umls-concept:C1515655
|
pubmed:issue |
8
|
pubmed:dateCreated |
1989-9-7
|
pubmed:abstractText |
The synthesis of a series of novel substituted hydroxamates has been described along with their profile of inhibitory activity against 5-lipoxygenase, 12-lipoxygenase, and cyclooxygenase enzymes. The structure--activity relationship suggests that future molecules could be designed to specifically inhibit one or more of these enzymes since there were definite differences in structure--activity relationships for these different enzymes. A representative number of these compounds have been tested in vivo and found to possess potent oral activity in a systemic anaphylaxis model mediated by leukotrienes and topical activity in an arachidonic acid induced inflammation model. One of these molecules, compound 20, demonstrated that a leukotriene antagonist pharmacophore can be modified such that it contains both antagonist activity and 5-lipoxygenase inhibitory activity.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Aug
|
pubmed:issn |
0022-2623
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
32
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
N
|
pubmed:pagination |
1836-42
|
pubmed:dateRevised |
2008-11-21
|
pubmed:meshHeading |
pubmed-meshheading:2502629-Anaphylaxis,
pubmed-meshheading:2502629-Animals,
pubmed-meshheading:2502629-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:2502629-Blood Platelets,
pubmed-meshheading:2502629-Chemical Phenomena,
pubmed-meshheading:2502629-Chemistry,
pubmed-meshheading:2502629-Cyclooxygenase Inhibitors,
pubmed-meshheading:2502629-Guinea Pigs,
pubmed-meshheading:2502629-Humans,
pubmed-meshheading:2502629-Hydroxamic Acids,
pubmed-meshheading:2502629-Leukotriene Antagonists,
pubmed-meshheading:2502629-Lipoxygenase Inhibitors,
pubmed-meshheading:2502629-Male,
pubmed-meshheading:2502629-Mice,
pubmed-meshheading:2502629-Neutrophils,
pubmed-meshheading:2502629-Rats,
pubmed-meshheading:2502629-Rats, Inbred Strains
|
pubmed:year |
1989
|
pubmed:articleTitle |
Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from platelets and their in vivo effects on inflammation and anaphylaxis.
|
pubmed:affiliation |
Rorer Central Research, Horsham, Pennsylvania 19044.
|
pubmed:publicationType |
Journal Article,
In Vitro
|