Acidic furo[3,2-b]indoles. A new series of potent antiallergy agents

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Abstract
A series of furo[3,2-b]indole carboxylic acids, tetrazoles and carbamoyltetrazoles was prepared and tested in vitro with use of a model of active pulmonary anaphylaxis, the modified Schultz-Dale Test (SDT). In this model, isolated guinea pig lung strips are repeatedly challenged with antigen in the presence of an antihistamine (H1). Most of the acidic furo[3,2-b]indoles tested inhibited the leukotriene-mediated lung contraction in a dose-related manner. Compounds with an N-phenyl substituent were more potent (IC50 [median inhibitory concentration] .ltoreq. 5.0 .mu.M) inhibitors of SDT than the N-methyl analogs (IC50 .gtoreq. 22.0 .mu.M). Most of the N-phenyl analogs were more potent in SDT than Fisons'' mediator-release inhibitor proxicromil (FPL-57,787; IC50 = 6.3 .mu.M). The most potent furo[3,2-b]indoles were those unsubstituted at C-7 and with N-phenyl, 2-carbamoyltetrazole and 3-alkoxy substituents. All of the carboxylic acid ester analogs tested were weak or inactive at concentrations of 10-30 .mu.M.

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