Design and Synthesis of Conformationally Constrained Analogs of 4-(3-Butoxy-4-methoxybenzyl) imidazolidin-2-one (Ro 20-1724) as Potent Inhibitors of cAMP- …

MF Brackeen, JA Stafford, DJ Cowan…

Index: Brackeen, Marcus F.; Cowan, David J.; Stafford, Jeffrey A.; Schoenen, Frank J.; Veal, James M.; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 24 p. 4848 - 4854

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Citation Number: 45

Abstract

The synthesis and biological evaluation of CAMP-specific phosphodiesterase (PDE IV) inhibitors is described. The PDE IV inhibitor 4-(3-butoxy-4-methoxybenzyl) imidazolidin-2- one(Ro 20-1724, 2) was used as a template from which to design a set of rigid oxazolidinones, imidazolidinones, and pyrrolizidinones that mimic Ro 20-1724 but differ in the orientation of the carbonyl group. The endo isomer of each of these heterocycles was ...