FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3025373131> ?p ?o ?g. }

• W3025373131 endingPage "1407" @default.
• W3025373131 startingPage "1398" @default.
• W3025373131 abstract "Abstract We report an extensive structure‐activity relationship optimization of polysubstituted pyrimidines that led to the discovery of 5‐butyl‐4‐(4‐benzyloxyphenyl)‐6‐phenylpyrimidin‐2‐amine, and its difluorinated analogue. These compounds are sub‐micromolar inhibitors of PGE 2 production (IC 50 as low as 12 nM). In order to identify the molecular target of anti‐inflammatory pyrimidines, we performed extensive studies including enzymatic assays, homology modeling and docking. The difluorinated analogue simultaneously inhibits two key enzymes of the arachidonic acid cascade, namely mPGES‐1 and COX‐2, with mPGES‐1 inhibition being the principal mechanism of action. Other pyrimidines studied are potent mPGES‐1 inhibitors with no observed inhibition of COX‐1/2 enzymes. Moreover, the two most potent compounds proved to be significantly effective in vivo in a model of acute inflammation, suppressing carrageenan‐induced rat paw edema by 36 and 46 %. The promising results of this study warrant further preclinical evaluation of selected anti‐inflammatory candidates." @default.
• W3025373131 created "2020-05-21" @default.
• W3025373131 creator A5000847224 @default.
• W3025373131 creator A5011128373 @default.
• W3025373131 creator A5026188443 @default.
• W3025373131 creator A5032881827 @default.
• W3025373131 creator A5042613113 @default.
• W3025373131 date "2020-06-04" @default.
• W3025373131 modified "2023-10-18" @default.
• W3025373131 title "Polysubstituted Pyrimidines as mPGES‐1 Inhibitors: Discovery of Potent Inhibitors of PGE₂ Production with Strong Anti‐inflammatory Effects in Carrageenan‐Induced Rat Paw Edema" @default.
• W3025373131 cites W1480874656 @default.
• W3025373131 cites W1488365705 @default.
• W3025373131 cites W1522220253 @default.
• W3025373131 cites W1573637659 @default.
• W3025373131 cites W1575542453 @default.
• W3025373131 cites W1855460106 @default.
• W3025373131 cites W1888068317 @default.
• W3025373131 cites W1969469655 @default.
• W3025373131 cites W1971957720 @default.
• W3025373131 cites W1980990431 @default.
• W3025373131 cites W1983292104 @default.
• W3025373131 cites W1983463925 @default.
• W3025373131 cites W1988055197 @default.
• W3025373131 cites W1988777700 @default.
• W3025373131 cites W1991038715 @default.
• W3025373131 cites W1992564723 @default.
• W3025373131 cites W1997106050 @default.
• W3025373131 cites W1998347942 @default.
• W3025373131 cites W1998959197 @default.
• W3025373131 cites W1999208772 @default.
• W3025373131 cites W2000724113 @default.
• W3025373131 cites W2003794633 @default.
• W3025373131 cites W2004572576 @default.
• W3025373131 cites W2007681746 @default.
• W3025373131 cites W2013096517 @default.
• W3025373131 cites W2013843777 @default.
• W3025373131 cites W2014449582 @default.
• W3025373131 cites W2014905802 @default.
• W3025373131 cites W2017092838 @default.
• W3025373131 cites W2020355467 @default.
• W3025373131 cites W2029133534 @default.
• W3025373131 cites W2030242710 @default.
• W3025373131 cites W2030793740 @default.
• W3025373131 cites W2039502840 @default.
• W3025373131 cites W2040399413 @default.
• W3025373131 cites W2047465266 @default.
• W3025373131 cites W2052031498 @default.
• W3025373131 cites W2053854129 @default.
• W3025373131 cites W2055447951 @default.
• W3025373131 cites W2056197566 @default.
• W3025373131 cites W2057573581 @default.
• W3025373131 cites W2061310202 @default.
• W3025373131 cites W2066837478 @default.
• W3025373131 cites W2075518489 @default.
• W3025373131 cites W2077629633 @default.
• W3025373131 cites W2077893896 @default.
• W3025373131 cites W2081521523 @default.
• W3025373131 cites W2082585817 @default.
• W3025373131 cites W2084353767 @default.
• W3025373131 cites W2087870536 @default.
• W3025373131 cites W2091769589 @default.
• W3025373131 cites W2106635797 @default.
• W3025373131 cites W2109372033 @default.
• W3025373131 cites W2109503514 @default.
• W3025373131 cites W2110902451 @default.
• W3025373131 cites W2118692983 @default.
• W3025373131 cites W2120112134 @default.
• W3025373131 cites W2136849767 @default.
• W3025373131 cites W2138249625 @default.
• W3025373131 cites W2142244748 @default.
• W3025373131 cites W2149083834 @default.
• W3025373131 cites W2156953939 @default.
• W3025373131 cites W2158960911 @default.
• W3025373131 cites W2165011857 @default.
• W3025373131 cites W2168398937 @default.
• W3025373131 cites W2178742227 @default.
• W3025373131 cites W2224870483 @default.
• W3025373131 cites W2274802250 @default.
• W3025373131 cites W2322441725 @default.
• W3025373131 cites W2325030053 @default.
• W3025373131 cites W2328732682 @default.
• W3025373131 cites W2329430018 @default.
• W3025373131 cites W2331395040 @default.
• W3025373131 cites W2335734535 @default.
• W3025373131 cites W2345021386 @default.
• W3025373131 cites W2395487850 @default.
• W3025373131 cites W2515017667 @default.
• W3025373131 cites W2554398789 @default.
• W3025373131 cites W2567420691 @default.
• W3025373131 cites W2610771026 @default.
• W3025373131 cites W2765330692 @default.
• W3025373131 cites W2790358550 @default.
• W3025373131 cites W2795166055 @default.
• W3025373131 cites W2806107014 @default.
• W3025373131 cites W2855363159 @default.
• W3025373131 cites W2883288032 @default.
• W3025373131 cites W2949206821 @default.
• W3025373131 cites W2953194867 @default.

• next