Details

Autor(en) / Beteiligte

• Gupta, Amit K.
• Varshney, Kanika
• Kumar, Vivek
• Srivastava, Kumkum
• Pant, Aditya B.
• Puri, Sunil K.
• Saxena, Anil K.

Titel

Design, Synthesis, and Biological Evaluation of Novel 1,2,4‐Trioxanes as Potential Antimalarial Agents

Ist Teil von

• Archiv der Pharmazie (Weinheim), 2017-04, Vol.350 (3-4), p.n/a

Ort / Verlag

Germany: Wiley Subscription Services, Inc

Erscheinungsjahr

2017

Quelle

Wiley-Blackwell Journals

Beschreibungen/Notizen

• A series of substituted 1,2,4‐trioxanes were synthesized and evaluated for their antimalarial potential, in silico ADME properties and cytotoxicity on neuronal cell lines. Among the 15 synthesized substituted 1,2,4‐trioxanes, two compounds (compound 15, IC50 = 25.71 nM; compound 21, IC50 = 19.6 nM) exhibited promising in vitro antimalarial potential comparable to those of the existing drugs chloroquine and artemisinin. Both of these compounds were found to be nontoxic up to 20 µM concentration in neuronal PC‐12 cells. Compound 21 may serve as an optimized lead compound because of its less in vitro toxicity and lower probability to cross the blood brain barrier. A series of substituted 1,2,4‐trioxanes were synthesized and evaluated for their antimalarial potential, ADME properties, and neuronal cell cytotoxicity. Two compounds (15, IC50 = 25.71 nM; 21, IC50 = 19.6 nM) showed in vitro antimalarial potential comparable to those of chloroquine and artemisinin. Due to its less toxicity and low probability to cross the blood brain barrier, compound 21 can be considered an optimized lead.