Medicinal Chemistry

Author(s): James W. Barlow, Tao Zhang, Orla Woods, Adam J. Byrne and John J. Walsh

DOI: 10.2174/157340611795564222

Novel Mast Cell-Stabilising Amine Derivatives of 3,4-Dihydronaphthalen-1(2H)-one and 6,7,8,9-Tetrahydro-5H-benzo[7]annulen-5-one

Page: [213 - 223] Pages: 11

  • * (Excluding Mailing and Handling)

Abstract

In an investigation of 4-amino-3,4-dihydronaphthalen-1(2H)-ones as novel modulators of allergic and inflammatory phenomena, we have investigated a series of cyclic analogues. Tertiary amines of structural types 9, 10, 20 and 21 were synthesised and evaluated for mast cell stabilising activity. In vitro and in vivo studies showed that of these compounds, the cyclohexenylamino derivatives of tetralone and benzosuberone of series 20 and 21 exhibited interesting activity both in vitro and in vivo.

Keywords: Anti-allergic, benzosuberone, mast cell, tetralone, 4-amino-3,4-dihydronaphthalen-1(2H)-ones, cyclic analogues, Tertiary amines, cyclohexenylamino derivatives, Stabilising Activity, Anaphylaxis