Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases

…, M Guala, I Peretto, E La Porta, PT Bolzoni…

Index: Armani, Elisabetta; Amari, Gabriele; Rizzi, Andrea; Fanti, Renato De; Ghidini, Eleonora; Capaldi, Carmelida; Carzaniga, Laura; Caruso, Paola; Guala, Matilde; Peretto, Ilaria; La Porta, Elena; Bolzoni, Pier T.; Facchinetti, Fabrizio; Carnini, Chiara; Moretto, Nadia; Patacchini, Riccardo; Bassani, Franco; Cenacchi, Valentina; Volta, Roberta; Amadei, Francesco; Capacchi, Silvia; Delcanale, Maurizio; Puccini, Paola; Catinella, Silvia; Civelli, Maurizio; Villetti, Gino Journal of Medicinal Chemistry, 2014 , vol. 57, # 3 p. 793 - 816

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Citation Number: 12

Abstract

The first steps in the selection process of a new anti-inflammatory drug for the inhaled treatment of asthma and chronic obstructive pulmonary disease are herein described. A series of novel ester derivatives of 1-(3-(cyclopropylmethoxy)-4-(difluoromethoxy) phenyl)-2- (3, 5-dichloropyridin-4-yl) ethanol have been synthesized and evaluated for inhibitory activity toward cAMP-specific phosphodiesterase-4 (PDE4). In particular, esters of ...