68256-19-9Relevant articles and documents
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases
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
supporting information, p. 793 - 816 (2014/03/21)
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 variously substituted benzoic acids were extensively explored, and structural modification of the alcoholic and benzoic moieties were performed to maximize the inhibitory potency. Several compounds with high activity in cell-free and cell-based assays were obtained. Through the evaluation of opportune in vitro ADME properties, a potential candidate suitable for inhaled administration in respiratory diseases was identified and tested in an in vivo model of pulmonary inflammation, proving its efficacy.
Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease
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, (2008/06/13)
The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Synthesis and Neuroleptic Activity of N--2-methoxy-5-sulfonamidobenzamides
Ogata, Masaru,Matsumoto, Hiroshi,Kida, Shiro,Shiomi, Teruo,Eigyo, Masami,Hirose, Katsumi
, p. 1137 - 1141 (2007/10/02)
A series of some novel N-benzamides involving replacement of the sulfamoyl group in sulpiride with a sulfonamido group was synthesized and tested for dopamine receptor blockade.In comparison with sulpiride, several compounds were considerably more potent than sulpiride as dopamine receptor blockers.The structure-activity relationships are discussed.