Discovery of fast-acting dual-stage antimalarial agents by profiling pyridylvinylquinoline chemical space via copper catalyzed azide-alkyne cycloadditions

G Huang, CM Solano, J Melendez, S Yu-Alfonzo… - European journal of …, 2021 - Elsevier
To identity fast-acting, multistage antimalarial agents, a series of pyridylvinylquinoline-
triazole analogues have been synthesized via CuAAC. Most of the compounds display …

Targeting Asexual and Sexual Blood Stages of the Human Malaria Parasite P. falciparum with 7‐Chloroquinoline‐Based 1,2,3‐Triazoles

I Wadi, D Prasad, N Batra, K Srivastava… - …, 2019 - Wiley Online Library
Abstract Novel 4‐amino‐7‐chloroquinoline‐based 1, 2, 3‐triazole hybrids were synthesised
in good yields by CuI‐catalysed Huisgen 1, 3‐dipolar cycloaddition reactions of 2‐azido‐N …

Property activity refinement of 2-anilino 4-amino substituted quinazolines as antimalarials with fast acting asexual parasite activity

TD Ashton, A Ngo, P Favuzza, HE Bullen… - Bioorganic …, 2021 - Elsevier
Malaria is a devastating disease caused by Plasmodium parasites. Emerging resistance
against current antimalarial therapeutics has engendered the need to develop antimalarials …

Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds

EM Guantai, K Ncokazi, TJ Egan, J Gut… - Bioorganic & medicinal …, 2010 - Elsevier
A targeted series of chalcone and dienone hybrid compounds containing aminoquinoline
and nucleoside templates was synthesized and evaluated for in vitro antimalarial activity …

N‐Cinnamoylation of Antimalarial Classics: Quinacrine Analogues with Decreased Toxicity and Dual‐Stage Activity

A Gomes, B Pérez, I Albuquerque, M Machado… - …, 2014 - Wiley Online Library
Plasmodium falciparum, the causative agent of the most lethal form of malaria, is becoming
increasingly resistant to most available drugs. A convenient approach to combat parasite …

Synthesis, structure–activity relationship, and antimalarial efficacy of 6-chloro-2-arylvinylquinolines

G Huang, C Murillo Solano, J Melendez… - Journal of medicinal …, 2020 - ACS Publications
There is an urgent need to develop new efficacious antimalarials to address the emerging
drug-resistant clinical cases. Our previous phenotypic screening identified styrylquinoline …

Synthesis of new 4-aminoquinolines and quinoline–acridine hybrids as antimalarial agents

A Kumar, K Srivastava, SR Kumar, SK Puri… - Bioorganic & medicinal …, 2010 - Elsevier
Despite emergence of resistance to CQ and other 4-aminoquinoline drugs in most of the
endemic regions, research findings provide considerable support that there is still significant …

Artemisinin–(Iso) quinoline Hybrids by C− H Activation and Click Chemistry: Combating Multidrug‐Resistant Malaria

A Çapcı, MM Lorion, H Wang, N Simon… - Angewandte Chemie …, 2019 - Wiley Online Library
A substantial challenge worldwide is emergent drug resistance in malaria parasites against
approved drugs, such as chloroquine (CQ). To address these unsolved CQ resistance …

Looking for new antiplasmodial quinazolines: DMAP-catalyzed synthesis of 4-benzyloxy-and 4-aryloxy-2-trichloromethylquinazolines and their in vitro evaluation …

A Gellis, N Primas, S Hutter, V Remusat… - European journal of …, 2016 - Elsevier
A DMAP catalyzed synthesis of new 4-benzyloxy-and 4-aryloxy-2-
trichloromethylquinazolines was studied, in a view to react 4-chloroquinazolines with poorly …

Synthesis, anti-plasmodial activities, and mechanistic insights of 4-aminoquinoline-triazolopyrimidine hybrids

S Chowdhary, Shalini, J Mosnier, I Fonta… - ACS Medicinal …, 2022 - ACS Publications
In the search of new antiplasmodial agents, a multitargeted approach was used in the
synthesis of triazolopyrimidine-and 4-aminoquinolines-based hybrids. In vitro antiplasmodial …