A series of 1, 2-coupled indane dimers with mast cell stabilisation and smooth muscle relaxation properties.
Asthma is characterised by bronchoconstriction and inflammation, with infiltration and activation of inflammatory cells such as eosinophils and mast cells, and subsequent release of inflammatory mediators. Much of the therapy directed at the treatment of asthma is either to provide symptomatic relief through bronchodilation or to reduce inflammation to prevent or delay airway remodelling. In an attempt to address both of these issues, a novel series of 1,2-indane dimers has been synthesized and evaluated for smooth muscle relaxant and mast cell stabilising activities. We have identified two lead compounds, 5 and 15, which have substantial mast cell stabilisation activity.
Trinity College Dublin, Department of Pharmacy and Pharmaceutical Sciences, Panoz Institute, Westland Row, Dublin 2, Ireland. hsheridn@tcd.ie
H
H
Sheridan
J J
JJ
Walsh
M
M
Jordan
C
C
Cogan
N
N
Frankish
D000818:Animals; D019281:Dimerization; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000502:physiology; D007189:Indans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D008407:Mast Cells / Q000502:physiology*; D015394:Molecular Structure; D009126:Muscle Relaxation / Q000502:physiology*; D009130:Muscle, Smooth / Q000502:physiology*
D007189:Indans