Discovery and preliminary structure–activity relationship analysis of 1, 14-sperminediphenylacetamides as potent and selective antimalarial lead compounds

LPP Liew, M Kaiser, BR Copp - Bioorganic & medicinal chemistry letters, 2013 - Elsevier
Screening of synthesized and isolated marine natural products for in vitro activity against
four parasitic protozoa has identified the ascidian metabolite 1, 14 …

Synthesis and in vitro and in vivo evaluation of antimalarial polyamines

LPP Liew, AN Pearce, M Kaiser, BR Copp - European journal of medicinal …, 2013 - Elsevier
Abstract We recently reported that 1, 14-diphenylacetamide derivatives of spermine exhibit
potent nM in vitro growth inhibition properties of Plasmodium falciparum. In an effort to …

Substituted aminoacetamides as novel leads for malaria treatment

NR Norcross, C Wilson, B Baragaña… - …, 2019 - Wiley Online Library
Herein we describe the optimization of a phenotypic hit against Plasmodium falciparum
based on an aminoacetamide scaffold. This led to N‐(3‐chloro‐4‐fluorophenyl)‐2‐methyl‐2 …

N-Aryl-2-aminobenzimidazoles: Novel, Efficacious, Antimalarial Lead Compounds

S Ramachandran, S Hameed P… - Journal of Medicinal …, 2014 - ACS Publications
From the phenotypic screening of the AstraZeneca corporate compound collection, N-aryl-2-
aminobenzimidazoles have emerged as novel hits against the asexual blood stage of …

3-Hydroxy-propanamidines, a new class of orally active antimalarials targeting Plasmodium falciparum

TC Knaab, J Held, BB Burckhardt… - Journal of medicinal …, 2021 - ACS Publications
3-Hydroxypropanamidines are a new promising class of highly active antiplasmodial agents.
The most active compound 22 exhibited excellent antiplasmodial in vitro activity with …

Discovery of a novel lead structure for anti-malarials

J Wiesner, P Wißner, HM Dahse, H Jomaa… - Bioorganic & medicinal …, 2001 - Elsevier
From a library of 61 compounds available from former studies 2, 5-bis-
acylaminobenzophenone 7p was identified as a lead structure for a novel class of anti …

The discovery, synthesis and antimalarial evaluation of natural product-based polyamine alkaloids

V Choomuenwai, BD Schwartz, KD Beattie… - Tetrahedron …, 2013 - Elsevier
Bioassay-guided fractionation of an antimalarial extract derived from the fungus Ramaria
subaurantiaca afforded the known polyamine alkaloid, pistillarin. Nine pistillarin analogues …

Aminoazabenzimidazoles, a novel class of orally active antimalarial agents

S Hameed P, M Chinnapattu, G Shanbag… - Journal of Medicinal …, 2014 - ACS Publications
Whole-cell high-throughput screening of the AstraZeneca compound library against the
asexual blood stage of Plasmodium falciparum (Pf) led to the identification of amino …

Interrogating alkyl and arylalkylpolyamino (bis) urea and (bis) thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium …

BK Verlinden, M De Beer, B Pachaiyappan… - Bioorganic & medicinal …, 2015 - Elsevier
A new series of potent potent aryl/alkylated (bis) urea-and (bis) thiourea polyamine
analogues were synthesized and evaluated in vitro for their antiplasmodial activity. Altering …

[HTML][HTML] Discovery of antiplasmodial pyridine carboxamides and thiocarboxamides

A Redway, C Spry, A Brown, U Wiedemann… - International Journal for …, 2024 - Elsevier
Malaria continues to be a significant burden, particularly in Africa, which accounts for 95% of
malaria deaths worldwide. Despite advances in malaria treatments, malaria eradication is …