Trimethoprim
- BP-S-6-Medicinal Chemistry III
- 2 hours ago
- 1 min read
Chemical Structure / Formula of Trimethoprim
Formula: C14H18N4O3
Structure: Pyrimidine derivative.

Mechanism of Action
Inhibits dihydrofolate reductase (DHFR), blocking bacterial DNA synthesis.
Uses
UTIs, respiratory tract infections (combined with sulfamethoxazole = Cotrimoxazole).
Side Effects
Megaloblastic anemia, hyperkalemia, GI upset.
Synthesis of Trimethoprim

Structure-Activity Relationship (SAR) of Trimethoprim
Structural Feature | SAR Insight |
2,4-diaminopyrimidine ring | Essential for binding to dihydrofolate reductase (DHFR). |
Substituted benzyl group | Increases selectivity for bacterial over human DHFR. |
Electron-donating groups (methoxy) | Improve potency and enhance lipophilicity. |
Bulky side chains | May hinder target binding or reduce specificity. |