Inhibitors of dihydrofolate reductase: Design, synthesis and antimicrobialactivities of 2,4-diamino-6-methyl-5-ethynylpyrimidines

Authors
Jones, ML Baccanari, DP Tansik, RL Boytos, CM Rudolph, SK Kuyper, LF
Citation
Ml. Jones et al., Inhibitors of dihydrofolate reductase: Design, synthesis and antimicrobialactivities of 2,4-diamino-6-methyl-5-ethynylpyrimidines, J HETERO CH, 36(1), 1999, pp. 145-148
Citations number
29
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
JOURNAL OF HETEROCYCLIC CHEMISTRY
ISSN journal
0022152X → ACNP
Volume
36
Issue
1
Year of publication
1999
Pages
145 - 148
Database
ISI
SICI code
0022-152X(199901/02)36:1<145:IODRDS>2.0.ZU;2-H
Abstract
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 s howed in vitro activity against several species of opportunistic fungi and the protozoan Toxoplasma gondii.