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6-methyl-5-[3-methyl-3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine
- Development stage
- Preclinical
- Lead developer
- University of Connecticut
- Modality
- Small Molecules
01
Overview
6-methyl-5-[3-methyl-3-(3,4,5-trimethoxyphenyl)but‑1‑yn‑1‑yl]pyrimidine‑2,4‑diamine is an experimental small molecule antifolate. It is a propargyl-linked analog designed to inhibit dihydrofolate reductase (DHFR), an enzyme critical for folate metabolism and DNA synthesis. The compound has demonstrated potent inhibitory activity against DHFR from multiple species including human (IC50 ≈ 290 nM), yeast (IC50 ≈ 11 nM), and Bacillus anthracis (IC50 ≈ 12.7 μM). Structural studies have shown it binds in the active site of DHFR from Candida albicans and related species[5][7]. This compound has not been approved for clinical use or entered advanced clinical trials; its primary application is as a research tool in the development of selective antifolates targeting fungal or microbial DHFR[2][8].
- Other names
- 6-Methyl-5-(3-methyl-3-(3,4,5-trimethoxyphenyl)but-1-ynyl)pyrimidine-2,4-diamine
02
Targets
DHFR (Dihydrofolate reductase)
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