Linked Life Data

2054858

Source:http://linkedlifedata.com/resource/pubmed/id/2054858

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1991-7-26
pubmed:abstractText
With partially purified kidney dehydropeptidase-I (DHP-I) preparations, the hydrolysis kinetics of glycyldehydrophenylalanine (Gly-dPh) by DHP-I were found to be completely non-Michaelian, whereas those of PS-5 and imipenem were composed of at least two-phase reactions which were also observed using Bacillus cereus type II beta-lactamase. Thus the DHP-I stabilities of 34 PS-5 carbapenem derivatives which were synthesized by chemical modification at the C-3 side chain of PS-5 were examined in vitro using fresh mouse, dog and human DHP-I preparations, and are tentatively expressed in reference to the DHP-I stabilities of PS-5. The in vitro DHP-I stability of PS-5 was significantly improved by introduction of basic side chains and cysteines at C-3. More particularly, the D-cysteinyl side chain was more stable relative to DHP-I than the L-cysteinyl. In vivo, however, the degree of improvement of the DHP-I-stability by chemical modification at C-3 was not sufficient enough to establish therapeutically effective levels of serum concentrations and urinary recoveries of the carbapenem derivatives after parenteral administration.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0009-2363
pubmed:author
pubmed:issnType
Print
pubmed:volume
39
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
341-8
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1991
pubmed:articleTitle
Kinetic analysis of dehydropeptidase-I and comparative in vitro and in vivo stabilities of PS-5 derivatives modified at the C-3 side chain.
pubmed:affiliation
MERCIAN Corporation, Central Research Laboratories, Fujisawa, Japan.
pubmed:publicationType
Journal Article, Comparative Study