Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
7802573 | European Journal of Medicinal Chemistry | 2012 | 10 Pages |
Abstract
⺠An improved synthesis of 2,4-diaminopyrimidine-based antibiotics is reported. ⺠Antibiotic synthesis includes a novel sealed-tube Heck reaction. ⺠The agents synthesized show activity in the μg/mL range. ⺠The size and planarity of the phthalazine C-1 substituent influences the activity. ⺠Steric and electronic factors affect the binding of the agents to DHFR.
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Authors
Baskar Nammalwar, Richard A. Bunce, K. Darrell Berlin, Christina R. Bourne, Philip C. Bourne, Esther W. Barrow, William W. Barrow,