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Inhibitors of dihydrofolate reductase: Design, synthesis and antimicrobial activities of 2,4‐diamino‐6‐methyl‐5‐ethynylpyrimidines
Author(s) -
Jones Michael L.,
Baccanari David P.,
Tansik Robert L.,
Boytos Christine M.,
Rudolph Sharon K.,
Kuyper Lee F.
Publication year - 1999
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.5570360122
Subject(s) - chemistry , dihydrofolate reductase , antimicrobial , in vitro , toxoplasma gondii , stereochemistry , pyrimidine , enzyme , biochemistry , organic chemistry , antibody , immunology , biology
Novel 2,4‐diamino‐6‐methyl‐5‐ethynylpyrimidines were prepared via palladium catalyzed coupling of 2,4‐diamino‐5‐iodo‐6‐methyl‐pyrimidine with terminal acetylenes. The compounds were inhibitors of dihydrofolate reductase and showed in vitro activity against several species of opportunistic fungi and the protozoan Toxoplasma gondii.