4-Nitro Styrylquinoline Is An Antimalarial Inhibiting Multiple Stages Of Plasmodium Falciparum Asexual Life Cycle

Keywords

Antimalarials; Antiplasmodials; Invasion inhibitor; Natural-product-like compounds; Styrylquinoline

Abstract

Drugs against malaria are losing their effectiveness because of emerging drug resistance. This underscores the need for novel therapeutic options for malaria with mechanism of actions distinct from current antimalarials. To identify novel pharmacophores against malaria we have screened compounds containing structural features of natural products that are pharmacologically relevant. This screening has identified a 4-nitro styrylquinoline (SQ) compound with submicromolar antiplasmodial activity and excellent selectivity. SQ exhibits a cellular action distinct from current antimalarials, acting early on malaria parasite's intraerythrocytic life cycle including merozoite invasion. The compound is a fast-acting parasitocidal agent and also exhibits curative property in the rodent malaria model when administered orally. In this report, we describe the synthesis, preliminary structure-function analysis, and the parasite developmental stage specific action of the SQ scaffold.

Publication Date

4-1-2017

Publication Title

International Journal for Parasitology: Drugs and Drug Resistance

Volume

7

Issue

1

Number of Pages

120-129

Document Type

Article

Personal Identifier

scopus

DOI Link

https://doi.org/10.1016/j.ijpddr.2017.02.002

Socpus ID

85014848604 (Scopus)

Source API URL

https://api.elsevier.com/content/abstract/scopus_id/85014848604

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