Folate antagonists. 17. Synthesis and biological properties of a 2,4-diamino-6-thioquinazoline analog of aminopterin |
| |
Authors: | Leslie M Werbel Linda Newton Edward F Elslager |
| |
Abstract: | A multistep route for the synthesis of N-4-(2,4-diamino-6-quinazolinyl)thio]benzoyl]-L-glutamic acid (2) from 4-mercaptobenzoic acid and 5-chloro-2-nitrobenzonitrile is described. Although this aminopterin analog lacked significant antimalarial activity, it was a potent inhibitor of dihydrofolate reductase from Trypanosoma cruzi. The pteroic ester analog 11 , however, was active against Plasmodium berghei infections in mice at high doses. |
| |
Keywords: | |
|
|