Discovery of dual target inhibitors against cyclooxygenases and leukotriene A4 hydrolyase

Z Chen, Y Wu, Y Liu, S Yang, Y Chen…

Index: Chen, Zheng; Wu, Yiran; Liu, Ying; Yang, Suijia; Chen, Yunjie; Lai, Luhua Journal of Medicinal Chemistry, 2011 , vol. 54, # 10 p. 3650 - 3660

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Citation Number: 22

Abstract

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 ...