Structure-activity relationships of antimalarial indolo [3, 2-c] quinolines [1, 2]

LM Werbel, SJ Kesten, WR Turner

Index: Werbel, L. M.; Kesten, S. J.; Turner, W. R. European Journal of Medicinal Chemistry, 1993 , vol. 28, # 11 p. 837 - 852

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Citation Number: 24

Abstract

Abstract Structure-activity relationships have been ascertained and chemical methodology developed for a series of antimalarial 3-chloroindolo [3, 2-c] quinoline-5-oxides. The basic side chain as well as the ring N-oxide are critical for antimalarial activity as is a bromine or chlorine in position 3. Substitution at positions 7, 8, 9, 10 is not essential, although the most potent analog in our studies was the 8-nitro compound 4vv.