Design, synthesis, and in vivo evaluation of oxamniquine methacrylate and acrylamide prodrugs.

Article Details

Citation
Copy to clipboard

Filho RP, de Souza Menezes CM, Pinto PL, Paula GA, Brandt CA, da Silveira MA

Design, synthesis, and in vivo evaluation of oxamniquine methacrylate and acrylamide prodrugs.

Bioorg Med Chem. 2007 Feb 1;15(3):1229-36. Epub 2006 Nov 16.

PubMed ID
17134907 [ View in PubMed
]
Abstract

Oxamniquine is an antiparasitic agent commonly used in therapeutics against Schistosoma mansoni. Although it is well tolerated, some adverse effects justify the search for new compounds with prolonged biological action, so that monomeric and polymeric oxamniquine prodrugs were designed. Synthetic results assisted by molecular modeling study showed the possibility to obtain the corresponding monomeric forms of the oxamniquine methacrylate (1) and oxamniquine acrylamide (2). Successful copolymerization procedure only occurred on the methacrylic compound, generating the oxamniquine methacrylate copolymer (3). Submitted to a preliminary in vivo biological evaluation, a similar oxamniquine profile was observed to the monomeric forms although an inadequate drug release may be responsible for the methacrylic copolymer failure.

DrugBank Data that Cites this Article

Drugs