Biological and Medicinal Chemistry

Therapeutic Potency of Mono and Diprenylated Acetophenone: A Case Study of in-vivo Antimalarial Evaluation

Authors

Abstract

Malaria remains a febrile infection of public health concern in many countries especially tropical countries in Africa, and certain countries in Southern and North America such as Brazil, Costa Rica, Mexico, Dominican Republic, Colombia, and Ecuador. Hence this has made research into this area paramount. Acetophenones are active fragments in many compounds with promising antimalarial activity, such as chalcones. In this study, 3,5-diprenyl acetophenone (I) and 5-diprenyl (II) acetophenone were synthesized using an aromatic substitution reaction and tested for in-vivo antimalarial activity. The in-vivo antimalarial potential of the synthesized compounds was carried out using a curative model with plasmodium berghei infected mice. At all the three doses tested; 25 mgkg-1, 50 mgkg-1 and 100 mgkg-1 3,5-diprenyl acetophenone (I) showed promising activity with percentage inhibition of 68.03%, 65.16% and 69.75% respectively demonstrating dose-dependent activity. However, 5-prenyl acetophenone (II) only displayed significant activity (72.12% inhibition) at a dose of 100 mgkg-1. The two compounds passed Lipinski’s rule of five and thus drug-like candidates.

Content

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