83642-37-9Relevant academic research and scientific papers
Discovery of dual target inhibitors against cyclooxygenases and leukotriene A4 hydrolyase
Chen, Zheng,Wu, Yiran,Liu, Ying,Yang, Suijia,Chen, Yunjie,Lai, Luhua
experimental part, p. 3650 - 3660 (2011/07/08)
Dual target inhibitors against COX-2 and LTA4H were designed by adding functional groups from a marketed COX-2 inhibitor, Nimesulide, to an existing LTA4H inhibitor 1-(2-(4-phenoxyphenoxy) ethyl) pyrrolidine. A series of phenoxyphenyl pyrrolidine compounds were synthesized and tested for their inhibition activities using enzyme assays and human whole blood assay. Introduction of small electron withdrawing groups like NO2 and CF3 in the ortho-position of the terminal phenyl ring was found to change the original single target LTA4H inhibitor to dual target LTA4H and COX-2 inhibitors. Compound 5a and 5m showed dual LTA 4H and COX-2 inhibition activities in the enzyme assays and the HWB assay with IC50 values in the micromolar to submicromolar range. As their activities in HWB assay were comparable to the two starting single target inhibitors, the two compounds are promising for further studies. The strategy used in the current study may be generally applicable to other dual target drug designs.
Sulfur-substituted diphenyl ethers having antiviral activity
-
, (2008/06/13)
Novel compounds exhibiting antiviral activity are disclosed, such compounds are represented by the formula: STR1 wherein m represents the integer 0, 1 or 2; R represents trihalomethyl, alkyl or phenyl; R1 represents hydrogen, bromo, chloro, fluoro, cyano, nitro, amino, alkyl, alkoxy or trifluoromethyl; R2 represents hydroxyl, bromo, chloro, fluoro, cyano, acetyl, benzoyl, substituted benzoyl, alkyl, alkoxy, substituted alkoxy, benzyl, substituted benzyl, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, or the radical --O(CH2)n R4 wherein n represents the integer 1, 2 or 3 and R4 represents cyano or dialkylamino; R3 represents hydrogen, hydroxyl, bromo, chloro, fluoro, cyano, acetyl, benzoyl, substituted benzoyl, alkyl, alkoxy, substituted alkoxy, benzyl, substituted benzyl, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, or the radical --O(CH2)n R4 wherein n represents the integer 1, 2 or 3; and R4 represents cyano or dialkylamino; or alternatively R2 and R3 taken together represent the radical --O--C(X)2 --O-- wherein X represents hydrogen, bromo, chloro or fluoro. Methods of using the above-noted compounds and structurally related compounds to employ their antiviral activity are also disclosed as well as pharmaceutically-acceptable compositions.
