Design, synthesis, and computational affinity prediction of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii
✍ Scribed by Malin Graffner-Nordberg; Karin Kolmodin; Johan Åqvist; Sherry F Queener; Anders Hallberg
- Book ID
- 113591314
- Publisher
- Elsevier Science
- Year
- 2004
- Tongue
- English
- Weight
- 222 KB
- Volume
- 22
- Category
- Article
- ISSN
- 0928-0987
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Nonclassical 2,4-Diamino-5-aryl-6-ethylpyrimidine Antifolates: Activity as Inhibitors of Dihydrofolate Reductase from Pneumocystis carinii and Toxoplasma gondii and as Antitumor Agents. -Title compounds such as (I) exhibit potent inhibitory activity against dihydrofolate reductase (DHFR) from Toxop
## Abstract The synthesis of four previously undescribed 2,4‐diaminopyrido[2,3‐__d__]pyrimidines (**3,4**) and 2,4‐diaminoquinazolines (**5,6**) with a bulky tricyclic aromatic group at the 6‐position is described. Condensation of dibenz[__b,f__]azepine with 2,4‐diamino‐6‐bromomethylpyrido[2,3‐__d_