Source:http://linkedlifedata.com/resource/pubmed/id/11310597
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
2001-4-19
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pubmed:abstractText |
The preparation and the pharmacological screening of novel anti-aggregatory/antiphlogistic polycyclic pyrimidine derivatives are described. The compounds were developed starting from bioactive 2-aminobenzopyranopyrimidine derivatives in order to assess the importance of the benzopyrano[4,3-d]pyrimidine structure and the role of an amino basic moiety in position 2. Antiplatelet activity was assessed in vitro against ADP and arachidonic acid-induced aggregation in guinea-pig plasma. Anti-inflammatory/analgesic/antipyretic activities were studied in rat paw oedema, mouse writhing test and E. coli-induced rat fever. Ulcerogenic and gastroprotective effects were also investigated in vivo on rat gastric mucosa. Among the tested compounds, the 5-substituted benzopyranopyrimidine derivatives 3d and 4d proved to be the most active antiplatelet agents as potent as acetylsalicylic acid against arachidonic acid-stimulated aggregation. Furthermore the 2-methylthio derivative 4d was endowed with greater efficacy against ADP aggregation suggesting that additional non-TXA2 dependent mechanisms are involved in its biological activity. Orally administered at 100 mg kg(-1) in rats this latter compound displayed antiphlogistic acitivity comparable to indomethacin (10 mg kg(-1)) coupled with an unusual gastroprotective effect on ethanol-induced ulcers. In conclusion, these findings indicate that the 5-pyrrolidino-2-methylthiobenzopyrano[4,3-d]pyrimidine 4d fulfils the chemical requirements to exhibit antiplatelet activity associated with gastroprotective effect.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics,
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, Non-Narcotic,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Inflammatory Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Aggregation Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Polycyclic Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
9
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
629-36
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11310597-Analgesics,
pubmed-meshheading:11310597-Analgesics, Non-Narcotic,
pubmed-meshheading:11310597-Animals,
pubmed-meshheading:11310597-Anti-Inflammatory Agents,
pubmed-meshheading:11310597-Drug Evaluation, Preclinical,
pubmed-meshheading:11310597-Gastric Mucosa,
pubmed-meshheading:11310597-Guinea Pigs,
pubmed-meshheading:11310597-Inhibitory Concentration 50,
pubmed-meshheading:11310597-Mice,
pubmed-meshheading:11310597-Platelet Aggregation,
pubmed-meshheading:11310597-Platelet Aggregation Inhibitors,
pubmed-meshheading:11310597-Polycyclic Compounds,
pubmed-meshheading:11310597-Pyrimidines,
pubmed-meshheading:11310597-Rats,
pubmed-meshheading:11310597-Structure-Activity Relationship
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pubmed:year |
2001
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pubmed:articleTitle |
New polycyclic pyrimidine derivatives with antiplatelet in vitro activity: synthesis and pharmacological screening.
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pubmed:affiliation |
Dipartimento di Scienze Farmaceutiche, Università degli Studi, Genova, Italy.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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