Journal of Medicinal Chemistry p. 1065 - 1070 (1983)
Update date:2022-08-04
Topics:
Metz
Pindell
Chen
4-[(p-Chlorophenoxy)acetyllamino]-5-chloro-2-methoxy-N-[2-(diethylamino)ethyl]benzamide (cloxacepride) exhibited substantial oral antiallergic potential in a reaginic PCA test in rats over a wide range of antigenic challenge times. Available reference compounds with oral activity, such as doxantrazole and 7-(2-hydroxyethoxy)-9-oxo-xanthene-2-carboxylic acid (AH 7725, 4) were active only when administered 15 min before challenge: 4, in particular, was not consistent in effect. Oral ED50 values for cloxacepride of 46-49 mg/kg were comparable to that of theophylline and to an intravenous injection of 2 mg/kg of disodium chromoglycate (DSCG) followed by immediate challenge. Following oral ED50 doses, 1 showed slower onset and longer duration of action than theophylline. The absence of inhibition of systemic anaphylaxis and of antihistaminic activity suggests specific effect for reaginic antigen antibody reactions. Structure-activity relationships of various chemical modifications were investigated and discussed in terms of essential substituents.
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(1981)Doi:10.1016/S0040-4039(01)00676-1
(2001)Doi:10.1039/DT9790000536
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(1979)