Linked Life Data

10488246

Source:http://linkedlifedata.com/resource/pubmed/id/10488246

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
1999-11-24
pubmed:abstractText
Reaction of twenty aromatic/heterocyclic sulfonamides containing a free amino, imino, hydrazino or hydroxyl group, with tosyl isocyanate or 3,4-dichlorophenyl isocyanate afforded two series of derivatives containing arylsulfonylureido or diarylureido moieties in their molecule respectively. The new derivatives were assayed as inhibitors of three carbonic anhydrase (CA) isozymes, CA I, II (cytosolic forms) and IV (membrane-bound form). Potent inhibition was observed against all three isozymes but especially against CA I, which is generally 10-75 times less susceptible to inhibition by the classical sulfonamides in clinical use as compared to the other major red cell isozyme, CA II, or the membrane-bound one, CA IV. The derivatives obtained from tosyl isocyanate were generally more potent than the corresponding ones obtained from 3,4-dichlorophenyl isocyanate. This is the first reported example of selective inhibition of CA I and might lead to more selective drugs/diagnostic agents from this class of pharmacologically relevant compounds.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
8755-5093
pubmed:author
pubmed:issnType
Print
pubmed:volume
14
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
343-63
pubmed:dateRevised
2004-11-17
pubmed:meshHeading
pubmed:year
1999
pubmed:articleTitle
Carbonic anhydrase inhibitors. Arylsulfonylureido- and arylureido-substituted aromatic and heterocyclic sulfonamides: towards selective inhibitors of carbonic anhydrase isozyme I.
pubmed:affiliation
Università degli Studi, Laboratorio di Chimica Inorganica e Bioinorganica, Firenze, Italia.
pubmed:publicationType
Journal Article