Novel thiopyrano[3,2-b] and cycloalkeno[1,2-b]indole derivatives with highinhibitory properties in LTB4 production

Series of thiopyrano[3,2-b] and cycloalkeno[1,2-b]indoles were synthesized and evaluated in order to determine the necessary structural requirements f or high leukotrienes biosynthesis inhibition. In vitro experiments showed t hat compounds 11b and 12b belonging to the second series were the most acti ve and selective compounds on LTB4 production. Further in vivo investigatio ns have shown additional very significant activity in the acute phorbol est er induced mouse ear swelling which is predictive of potential antipsoriati c properties. (C) Elsevier, Paris.