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Synthesis of naphthyridinone derivatives as potential antimalarials
Author(s) -
Carroll F. Ivy,
Berrang Bertold D.,
Linn C. Preston
Publication year - 1981
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570180519
Subject(s) - chemistry , plasmodium berghei , amino acid , stereochemistry , alkyl , combinatorial chemistry , organic chemistry , biochemistry , malaria , immunology , biology
In this paper we present the synthesis of 8‐(4′‐amino‐1′methyl‐butylamino)‐5‐(β,β,β‐trifluoroethoxy)‐1,6‐naphthyridine ( 4 ), 8‐(4′‐amino‐1′methylbutylamino)‐6‐methyl‐1,6‐naphthyricline‐5‐one ( 5 ), two 1‐alkyl‐3‐(4′‐amino‐1′‐methylbutylamino)‐7‐methyl‐1,8‐naphthyridin‐4‐ones ( 20a ) and 20b ), 3‐(1′‐amino‐4′‐methylbutyl‐amino)‐l‐ethyl‐7‐methyl‐l,8‐naphthyridin‐4‐one (20c), and 4‐(4′‐diethylamino‐1′‐methylbutylamino)‐7‐methyl‐1,7‐naphthyridin‐8‐one ( 28 ). The compounds were evaluated for antimalarial activity in the Plasmodium berghei screen and found to be inactive.