pubmed-article:11310597 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:11310597 | lifeskim:mentions | umls-concept:C0220908 | lld:lifeskim |
pubmed-article:11310597 | lifeskim:mentions | umls-concept:C0441655 | lld:lifeskim |
pubmed-article:11310597 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
pubmed-article:11310597 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
pubmed-article:11310597 | lifeskim:mentions | umls-concept:C0205464 | lld:lifeskim |
pubmed-article:11310597 | lifeskim:mentions | umls-concept:C1533691 | lld:lifeskim |
pubmed-article:11310597 | lifeskim:mentions | umls-concept:C0034284 | lld:lifeskim |
pubmed-article:11310597 | lifeskim:mentions | umls-concept:C0243072 | lld:lifeskim |
pubmed-article:11310597 | pubmed:issue | 3 | lld:pubmed |
pubmed-article:11310597 | pubmed:dateCreated | 2001-4-19 | lld:pubmed |
pubmed-article:11310597 | 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. | lld:pubmed |
pubmed-article:11310597 | pubmed:language | eng | lld:pubmed |
pubmed-article:11310597 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11310597 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:11310597 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11310597 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11310597 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11310597 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11310597 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11310597 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:11310597 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:11310597 | pubmed:month | Mar | lld:pubmed |
pubmed-article:11310597 | pubmed:issn | 0968-0896 | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:ImpicciatoreM... | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:BondavalliFF | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:ChiavariniMM | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:RaniseAA | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:BarocelliEE | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:BallabeniVV | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:SchenoneSS | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:BrunoOO | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:BertoniSS | lld:pubmed |
pubmed-article:11310597 | pubmed:author | pubmed-author:TognoliniMM | lld:pubmed |
pubmed-article:11310597 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:11310597 | pubmed:volume | 9 | lld:pubmed |
pubmed-article:11310597 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:11310597 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:11310597 | pubmed:pagination | 629-36 | lld:pubmed |
pubmed-article:11310597 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
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pubmed-article:11310597 | pubmed:year | 2001 | lld:pubmed |
pubmed-article:11310597 | pubmed:articleTitle | New polycyclic pyrimidine derivatives with antiplatelet in vitro activity: synthesis and pharmacological screening. | lld:pubmed |
pubmed-article:11310597 | pubmed:affiliation | Dipartimento di Scienze Farmaceutiche, Università degli Studi, Genova, Italy. | lld:pubmed |
pubmed-article:11310597 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:11310597 | pubmed:publicationType | Comparative Study | lld:pubmed |
pubmed-article:11310597 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |