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Polysubstituted Pyrimidines as mPGES‐1 Inhibitors: Discovery of Potent Inhibitors of PGE 2 Production with Strong Anti‐inflammatory Effects in Carrageenan‐Induced Rat Paw Edema
Author(s) -
Kalčic Filip,
Kolman Viktor,
Ajani Haresh,
Zídek Zdeněk,
Janeba Zlatko
Publication year - 2020
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202000520
Subject(s) - arachidonic acid , cyclooxygenase , chemistry , enzyme , pharmacology , prostaglandin , thromboxane a2 , carrageenan , stereochemistry , prostaglandin e , biochemistry , medicine , receptor
The Front Cover illustrates the cyclooxygenase (COX) highway (pathway), a part of the arachidonic acid (AA) cascade, where prostaglandins (PGE 2 , PGI 2 , PGD 2 , and also PGF 2α ) and thromboxane TXA 2 are the major metabolites of AA. While inhibition of COX1/2 enzymes by NSAIDs or coxibs shuts down the whole COX highway (with some serious side‐effect consequences), some of the polysubstituted pyrimidines presented in our study are able to selectively inhibit the PGE 2 production, where the main molecular target of these compounds is mPGES‐1. (Design by Tomáš Belloň and Zlatko Janeba, IOCB.) More information can be found in the Full Paper by Zdeněk Zídek, Zlatko Janeba et al.