Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
22
pubmed:dateCreated
1995-12-26
pubmed:abstractText
Synthesis and structural requirements for good oral activity of a series of para-substituted benzoyl esters of 4-hydroxybenzamidine serine protease inhibitors are described. The structure required for good oral activity was found to be general formula II whose corresponding ester has to be hydrolyzed in the intestine before absorption through the mucous membranes or in plasma after absorption. Biological evaluation of oral absorption using plasma anti-trypsin activity was useful for rapid evaluation. By measuring their actual plasma concentrations after oral administration, compounds 14 and 16b were confirmed to show good area under the plasma concentration-time curves (AUC). Their plasma concentrations corresponded to their plasma anti-trypsin activity. Structure-oral activity relationships are discussed.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
27
pubmed:volume
38
pubmed:owner
NLM
pubmed:authorsComplete
N
pubmed:pagination
4508-17
pubmed:dateRevised
2003-11-14
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
New orally active serine protease inhibitors: structural requirements for their good oral activity.
pubmed:affiliation
Minase Research Institute, Ono Pharmaceutical Ltd., Osaka, Japan.
pubmed:publicationType
Journal Article