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

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. Substit...

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Bibliographic Details
Published inEuropean journal of medicinal chemistry Vol. 28; no. 11; pp. 837 - 852
Main Authors Werbel, LM, Kesten, SJ, Turner, WR
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Masson SAS 1993
Elsevier
Subjects
antimalarial agents
Chemistry
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings
indolo[3,2- c]quinolines [1, 2]
Organic chemistry
Preparations and properties
indolo[3,2- c]quinolines [1, 2]
antimalarial agents
Antimalarial
Vertebrata
Mammalia
Structure activity relation
Mouse
Nitrogen heterocycle
Nitrone
Rodentia
Aromatic compound
Tetracyclic compound
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Summary: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.
ISSN:0223-5234
1768-3254
DOI:10.1016/0223-5234(93)90036-E