Synthesis and antimicrobial activity of N(1)-benzyl or N(1)-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines.
Article Details
- CitationCopy to clipboard
Ma X, Tan ST, Khoo CL, Sim HM, Chan LW, Chui WK
Synthesis and antimicrobial activity of N(1)-benzyl or N(1)-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines.
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5428-31. doi: 10.1016/j.bmcl.2011.06.125. Epub 2011 Jul 2.
- PubMed ID
- 21788136 [ View in PubMed]
- Abstract
The emergence and spread of multidrug-resistant strains of Staphylococcus aureus and Mycobacterium tuberculosis are generating a threat to public health worldwide. In the current study, a series of N(1)-benzyl and N(1)-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamine derivatives were synthesized and investigated for their antimicrobial activity against S. aureus, and Mycobacterium smegmatis which is taxonomically related to M. tuberculosis. Most of the compounds exhibited good activity against M. smegmatis as determined by comparison of diameters of the zone of inhibition of test compounds and standard antibiotics. Compound 7o showed potent antimycobacterial activity against M. smegmatis without mammalian DHFR inhibition liability. The results from this study indicate that 1-benzyl derivatives of 1,6-dihydro-1,3,5-triazine-2,4-diamines may be used as lead compounds for the discovery of antimycobacterial agents.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Trimethoprim Dihydrofolate reductase IC 50 (nM) >100000 N/A N/A Details