New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents.

Ibrahim Radini,Emad El-Telbani,Tarek Elsheikh,Rizk Khidre

doi:10.3390/molecules21070909

Abstract

A novel series of dihydropyrimidines (DHPMs) 4a–j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesized quinoline derivatives against Plasmodium falciparum revealed them to possess moderate to high antimalarial activities, with IC50 values ranging from 0.014–5.87 μg/mL. Compounds 4b,g,i and 12 showed excellent antimalarial activity against to Plasmodium falciparum compared with the antimalarial agent chloroquine (CQ).

Highlights

Malaria is one of the principal diseases of the developing countries, in Africa, Asia and South America
Among five typically recognized Plasmodium species causing this disease in humans, Plasmodium falciparum is responsible for about 95% of worldwide malaria and has a mortality rate of 1%–3%, and Plasmodium vivax for most morbidity, representing a reservoir of latent infection that hampers current control and future elimination efforts [3,4,5,6]
A series of new quinoline derivatives has been synthesized starting from tetrazoloquinoline-3carbaldehyde, 2-oxo-1,2-dihydroquinoline-3-carbaldehyde, 2-chloroquinoline-3-carbaldehyde, and

Summary

Introduction

Malaria is one of the principal diseases of the developing countries, in Africa, Asia and South America. Among five typically recognized Plasmodium species causing this disease in humans, Plasmodium falciparum is responsible for about 95% of worldwide malaria and has a mortality rate of 1%–3%, and Plasmodium vivax for most morbidity, representing a reservoir of latent infection that hampers current control and future elimination efforts [3,4,5,6]. Plasmodium falciparum to known antimalarial agents demands a continuous effort to develop new antimalarial agents especially, as an effective vaccine for malaria is not available. Molecules 2016, 21, 909 several quinolines compounds and screened for their antimalarial activities. These compounds be active on the CQ-resistant strain FcB1 and could lead to the availability of better

Methods

Results

Conclusion