Synthesis and in Vitro and in Vivo Antimalarial Activity of N-(7-Chloro-4-quinolyl)-1, 4-bis (3-aminopropyl) piperazine Derivatives

A Ryckebusch, R Deprez-Poulain, L Maes… - Journal of medicinal …, 2003 - ACS Publications
Three series of monoquinolines consisting of a 1, 4-bis (3-aminopropyl) piperazine linker
and a large variety of terminal groups were synthesized. Our aim was to prove that in related …

Synthesis of novel triazole-linked mefloquine derivatives: Biological evaluation against Plasmodium falciparum

AR Hamann, C de Kock, PJ Smith… - Bioorganic & Medicinal …, 2014 - Elsevier
Abstract Using 2, 8-bis (trifluoromethyl) quinoline, the pharmacophore of mefloquine, as
scaffold, eleven novel triazole-linked compounds have been synthesised by the application …

Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against …

A Marwaha, J White, F El_Mazouni… - Journal of medicinal …, 2012 - ACS Publications
Plasmodium falciparum causes approximately 1 million deaths annually. However,
increasing resistance imposes a continuous threat to existing drug therapies. We previously …

Optimization of 2-anilino 4-amino substituted quinazolines into potent antimalarial agents with oral in vivo activity

PR Gilson, C Tan, KE Jarman, KN Lowes… - Journal of medicinal …, 2017 - ACS Publications
Novel antimalarial therapeutics that target multiple stages of the parasite lifecycle are
urgently required to tackle the emerging problem of resistance with current drugs. Here, we …

Pyrazole-pyrazoline as promising novel antimalarial agents: A mechanistic study

G Kumar, O Tanwar, J Kumar, M Akhter… - European journal of …, 2018 - Elsevier
A series of pyrazole-pyrazoline substituted with benzenesulfonamide were synthesized and
evaluated for their antimalarial activity in vitro and in vivo. The compounds were active …

Discovery of a quinoline-4-carboxamide derivative with a novel mechanism of action, multistage antimalarial activity, and potent in vivo efficacy

B Baragaña, NR Norcross, C Wilson… - Journal of medicinal …, 2016 - ACS Publications
The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-
carboxamides are described. This series was identified from a phenotypic screen against …

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 …

Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines

P Verhaeghe, N Azas, M Gasquet, S Hutter… - Bioorganic & Medicinal …, 2008 - Elsevier
A series of original 4-aryl-substituted 2-trichloromethylquinazoline derivatives was
synthesized using a microwave-assisted Suzuki-Miyaura cross-coupling approach …

Recent developments in antimalarial drug discovery

T Umumararungu, JB Nkuranga, G Habarurema… - Bioorganic & Medicinal …, 2023 - Elsevier
Although malaria remains a big burden to many countries that it threatens their socio-
economic stability, particularly in the countries where malaria is endemic, there have been …

Antimalarial activity and mechanisms of action of two novel 4-aminoquinolines against chloroquine-resistant parasites

ACC Aguiar, RM Santos, FJB Figueiredo… - PLoS …, 2012 - journals.plos.org
Chloroquine (CQ) is a cost effective antimalarial drug with a relatively good safety profile (or
therapeutic index). However, CQ is no longer used alone to treat patients with Plasmodium …