Dihydroethanoanthracene Derivatives as In Vitro Malarial Chloroquine Resistance Reversal Agents

Abstract

The ability of four 9,10-dihydroethanoanthracene derivatives (BG920, BG932, BG958, and BG996), as well as verapamil and promethazine, to reverse chloroquine resistance was assessed against 24 chloroquine-resistant and 10 chloroquine-susceptible strains of Plasmodium falciparum from different countries. The 9,10-dihydroethanoanthracene derivatives clearly increase chloroquine susceptibility only in chloroquine-resistant isolates

Pentacycloundecylamines and conjugates thereof as chemosensitizers and reversed chloroquine agents

“…Chemosensitizers are structurally diverse molecules that are known to reverse CQ resistance by inhibiting the p-glycoprotein efflux pump and/or the PfCQRT protein associated with CQ export from the digestive vacuole in CQ resistant parasites. [7][8][9] Chemosensitizers include the antihistaminic agent chlorpheniramine and calcium channel blockers such as imipramine and verapamil. These drugs have little or no inherent antimalarial activity but have shown to reverse CQ resistance in P. falciparum when co-administered with CQ.…”

Corrigendum: β‐Enaminonitriles in Heterocyclic Synthesis: Synthesis of New 1,4‐Dihydropyridine, Tetrahydropyridine, Nicotinonitrile and Aminopyrazole Derivatives

“…Also, the pyridine ring was found in the skeleton of many compounds that have potent antibacterial, antifungal and anticancer properties. 13,14 In addition, nitrogen-linked heterocyclic compounds received considerable attention in recent years because of their medicinal and pesticidal importance. 15,16 It is well known that the study of pyrazole derivatives is significant in pesticide chemistry, and some pyrazole derivatives were widely used because of their antiviral, 17 antitumor, 18 anti-inflammatory, 19 antibacterial, 20 herbi-cidal, 21 insecticidal, 22 and fungicidal activities.…”

Polymorphism in Plasmodium falciparum Drug Transporter Proteins and Reversal of In Vitro Chloroquine Resistance by a 9,10-Dihydroethanoanthracene Derivative

“…Several compounds, such as verapamil (VER) (15,22), desipramine (3,5), and antihistaminic drugs (13,18), have demonstrated in the past decade a promising capacity to reverse CQ resistance in parasite isolates in vitro, in animal models, and in human patients with malaria. The capacity of 9,10-dihydroethanoanthracenes to reverse the CQ resistance of several strains and isolates was shown previously (2,17,19,20).…”

“…The in vitro isotopic microtest used in this study was described previously (17). The IC 50 was determined by nonlinear regression analysis of log dose-response curves.…”