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Synthesis and antiplasmodial activity of novel 2,4-diaminopyrimidines.
| Publication Type | Journal Article |
| Authors | Martyn, DC, Nijjar A., Celatka CA, Mazitschek R., Cortese JF, Tyndall E., Liu H., Fitzgerald MM, O'Shea TJ, Danthi S., and Clardy J. |
| Abstract | Two sets of diaminopyrimidines, totalling 45 compounds, were synthesized and assayed against Plasmodium falciparum. The SAR was relatively shallow, with only the presence of a 2-(pyrrolidin-1-yl)ethyl group at R(2) significantly affecting activity. A subsequent series addressed high LogD values by introducing more polar side groups, with the most active compounds possessing diazepine and N-benzyl-4-aminopiperidyl groups at R(1)/R(2). A final series attempted to address high in vitro microsomal clearance by replacing the C6-Me group with CF(3), however antiplasmodial activity decreased without any improvement in clearance. The C6-CF(3) group decreased hERG inhibition, probably as a result of decreased amine basicity at C2/C4. |
| Year of Publication | 2010 |
| Journal | Bioorganic & medicinal chemistry letters |
| Volume | 20 |
| Issue | 1 |
| Pages | 228-31 |
| Date Published (YYYY/MM/DD) | 2010/01/01 |
| ISSN Number | 0960-894X |
| DOI | 10.1016/j.bmcl.2009.10.133 |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/19914064?dopt=Abstract |
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