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Letters in Drug Design & Discovery

Author(s): Jeewoo Lee, Su Yeon Kim, Hye Ra Lee and Je Hak Kim

DOI: 10.2174/1570180043485662

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SAR and Molecular Modeling of N-Benzyl-N-hydroxy-3-(cyclopentyloxy)-4- methoxybenzene Carboxamide Analogues as Potent Phosphodiesterase-4 Inhibitors

Page: [19 - 23] Pages: 5

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Abstract

A series of N-benzyl-N-hydroxy-3-(cyclopentyloxy)-4-methoxybenzene carboxamide analogues have been investigated as PDE4 inhibitors. Two compounds, 3- carboxylic (12b) and 3-hydroxamic acid (13b) derivatives, have shown potent inhibition toward PDE4, with IC50s of 0.114 and 0.047 μM, respectively. Docking of the compound 13b into the binding pocket of the PDE4 catalytic domain revealed interactions corresponding to those of the cAMP substrate.

Keywords: cyclopentyloxy, methoxybenzene, N-benzyl-N-hydroxy, 3-hydroxamic acid