Novel Thiopyrano[3,2-b] and Cycloalkeno[1,2-b]indole Derivatives with High Inhibitory Properties in LTB4 Production.

Abstract Series of thiopyrano[3,2- b ] and cycloalkeno[1,2- b ]indoles were synthesized and evaluated in order to determine thenecessary structural requirements for high leukotrienes biosynthesis inhibition. In vitro experiments showed that compounds 11b and 12b belonging to the second series were the most active and selective compounds on LTB 4 production. Further in vivo investigations have shown additional very significant activity in the acute phorbol ester induced mouse ear swelling which is predictive of potential antipsoriatic properties.