948049-20-5Relevant articles and documents
Orally active antimalarials: Synthesis and bioevaluation of a new series of steroid-based 1,2,4-trioxanes against multi-drug resistant malaria in mice
Singh, Chandan,Sharma, Upasana,Saxena, Gunjan,Puri, Sunil. K.
, p. 4097 - 4101 (2007)
A new series of steroid-based 1,2,4-trioxanes 7a-f, 8a-f and 9b-e have been synthesized and evaluated for their antimalarial activity against multi-drug resistant Plasmodium yoelii in Swiss mice by oral route. The biological activity shows a strong depend
Coumarin-trioxane hybrids: Synthesis and evaluation as a new class of antimalarial scaffolds
Sashidhara, Koneni V.,Kumar, Abdhesh,Dodda, Ranga Prasad,Krishna, Naikade Niraj,Agarwal, Pooja,Srivastava, Kumkum,Puri
, p. 3926 - 3930 (2012/07/03)
First synthesis of novel coumarin-trioxane hybrids is reported. The synthesis was achieved via condensation of β-hydroxyhydroperoxides with coumarinic-aldehydes in presence of p-toluenesulfonic acid in good yields and the novel hybrids were evaluated for
Bile acid-based 1,2,4-trioxanes: Synthesis and antimalarial assessment(1)
Singh, Chandan,Hassam, Mohammad,Verma, Ved Prakash,Singh, Ajit Shanker,Naikade, Niraj Krishna,Puri, Sunil K.,Maulik, Prakas R.,Kant, Ruchir
, p. 10662 - 10673 (2013/02/23)
A new series of bile acid-based trioxanes 23a-d, 24a-d, 25a-d, 26a, 26b, and 26d have been synthesized and assessed for their antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice by oral route. The antimalarial activity of these trioxanes showed a strong dependence on the side-chain length; shortening side-chain length lead to increase in activity. The antimalarial activity also showed even stronger dependence on the stereochemistry at C3 and C6 (C21 in Figure 5) of the trioxane moiety. Of the two diastereomers isolated of each of the trioxanes, more polar one was significantly more active than the less polar one. The more polar diastereomer of the trioxanes 26a, 26b, and 26d, were the most active compounds of the series. All these three trioxanes provided 100% protection at 24 mg/kg × 4 days. In this model β-arteether provided 100% and 20% protection at 48 mg/kg × 4 days and 24 mg/kg × 4 days, respectively.