|کد مقاله||کد نشریه||سال انتشار||مقاله انگلیسی||ترجمه فارسی||نسخه تمام متن|
|6481758||1401036||2016||15 صفحه PDF||سفارش دهید||دانلود رایگان|
- New aryl-substituted propanol derivatives (APD) show promising antimalarial activity.
- Î³-amino alcohol moiety is significant antimalarial chemotype.
- Compound 22 displays excellent inÂ vivo parasitemia reduction (98%) and complete cure.
- APD are active against drug sensitive and multidrug resistant strains.
Synthesis of new 1-aryl-3-substituted propanol derivatives followed by structure-activity relationship, in silico drug-likeness, cytotoxicity, genotoxicity, in silico metabolism, in silico pharmacophore modeling, and inÂ vivo studies led to the identification of compounds 22 and 23 with significant inÂ vitro antiplasmodial activity against drug sensitive (D6 IC50Â â¤Â 0.19Â Î¼M) and multidrug resistant (FCR-3 IC50Â â¤Â 0.40Â Î¼M and C235 IC50Â â¤Â 0.28Â Î¼M) strains of Plasmodium falciparum. Adequate selectivity index and absence of genotoxicity was also observed. Notably, compound 22 displays excellent parasitemia reduction (98Â Â±Â 1%), and complete cure with all treated mice surviving through the entire period with no signs of toxicity. One important factor is the agreement between inÂ vitro potency and inÂ vivo studies. Target exploration was performed; this chemotype series exhibits an alternative antimalarial mechanism.
Journal: International Journal for Parasitology: Drugs and Drug Resistance - Volume 6, Issue 3, December 2016, Pages 184-198