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Synthesis and Effects on the COX‐1 and COX‐2 Activity in Human Whole Blood ex vivo of Derivatives Containing the [1]Benzothienol‐[3, 2‐ d ]pyrimidin‐4‐one Heterocyclic System
Author(s) -
Santagati Andrea,
Granata Giuseppe,
Marrazzo Agostino,
Santagati Maria
Publication year - 2003
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200300753
Subject(s) - ex vivo , chemistry , in vivo , thromboxane , whole blood , thromboxane a2 , stereochemistry , derivative (finance) , thromboxane b2 , pharmacology , platelet , biochemistry , in vitro , medicine , biology , receptor , microbiology and biotechnology , economics , financial economics
Methyl and phenyl derivatives containing the [1]Benzothieno [3, 2‐ d ]pyrimidin‐4‐one system have been synthesized and tested as inhibitors of COX‐1 and COX‐2 activities in human whole blood (HWB) ex vivo ; all compounds turned out to be weak inhibitors of COX‐1 activity, as deduced from the TXB 2 (thromboxane B) generation; the acid phenyl derivative 11 b was an interesting inhibitor of COX‐2 activity, as deduced from the PGE 2 (prostaglandine E) generation.