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Updated: Jul 26, 2026

Optimized Griess Reaction for UV-Vis and Naked-eye Determination of Anti-malarial Primaquine
Published on: October 11, 2019
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials
N P Jensen1, A L Ager, R A Bliss
1Jacobus Pharmaceutical, Box 5290, Princeton, New Jersey 08540, USA. romich@aol.com
Abstract:
A total of 34 analogues of the biguanide PS-15 (5s), a prodrug of the diaminotriazine WR-99210 (8s), have been prepared. Several of them, such as 5b (PS-33) and 5m (PS-26), maintain or exceed the in vivo activity of PS-15 while not requiring the use of highly regulated starting materials. The putative diaminotriazine metabolites of these new analogues (compounds 8) have also been prepared and shown to maintain the activity against resistant P. falciparum strains. The structure-activity relationships of biguanides 5 and putative metabolites 8 are discussed.
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