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NOT Open Access | In vitro antiplasmodial activity, targeted LC-MS metabolite profiling, and identification of major natural products in the bioactive extracts of Palicourea and Psychotria species from the Amazonia and Atlantic Forest biomes, Brazil

September 7, 2021 - 15:32 -- NOT Open Access
Gontijo DC, do Nascimento MFA, Rody HVS, Magalhães RA, Margalho LF, Brandão GC, de Oliveira AB
Metabolomics. 2021 Sep 4;17(9):81

To assess the antiplasmodial activity of 24 extracts from Palicourea and Psychotria genera, along with the targeted LC–MS metabolite profiling, as well as identification of the main metabolites in the bioactive extracts.

Antiplasmodial and antileishmanial flavonoids from Mundulea sericea

March 3, 2021 - 16:51 -- Open Access
Chepkirui C, Ochieng PJ, Yenesew A, et al.
Fitoterapia. 2021 Mar;149:104796

Five known compounds (1-5) were isolated from the extract of Mundulea sericea leaves. Similar investigation of the roots of this plant afforded an additional three known compounds (6-8). The structures were elucidated using NMR spectroscopic and mass spectrometric analyses. The absolute configuration of 1 was established using ECD spectroscopy. In an antiplasmodial activity assay, compound 1 showed good activity with an IC50 of 2.0 μM against chloroquine-resistant W2, and 6.6 μM against the chloroquine-sensitive 3D7 strains of Plasmodium falciparum.

NOT Open Access | A Concise Total Synthesis of Dehydroantofine and the Antimalarial Activity against Chloroquine-Resistant P. falciparum

January 26, 2021 - 15:09 -- NOT Open Access
Yamasaki N, Iwasaki I, Sakumi K, Hokari R, Ishiyama A, Iwatsuki M, Nakahara M, Higashibayashi S, Sugai T, Imagawa H, Kubo M, Fukuyama Y, Ōmura S, Yamamoto H
Chemistry. 2021 Jan 2

A total synthesis of dehydroantofine was achieved by employing a novel, regioselective azahetero Diels-Alder reaction of the easily accessible 3,5-dichloro-2 H -1,4-oxazin-2-one with 4-ethynyl-1,2-dimethoxybenzene as a key step.

An open label study of the safety and efficacy of a single dose of weekly chloroquine and azithromycin administered for malaria prophylaxis in healthy adults challenged with 7G8 chloroquine-resistant Plasmodium falciparum in...

September 16, 2020 - 12:48 -- Open Access
Jeffrey Livezey, Patrick Twomey, Paige Waterman, et al.
Malaria Journal 2020 19:336, 16 September 2020

Malaria remains the top infectious disease threat facing the U.S. military in many forward operating environments. Compliance with malaria chemoprophylaxis remains a critical component in preventing malaria in the deployed Service Member. Studies of previous military operations show that compliance is consistently higher with weekly versus daily dosing regimens. Current FDA approved weekly chemoprophylaxis options have contraindications that can limit prescribing. The combination of chloroquine (CQ) with azithromycin (AZ) has previously been shown to be an efficacious treatment option for malaria, has pharmacokinetics compatible with weekly dosing, and has shown synergy when combined in vitro.

Global assessment of genetic paradigms of Pvmdr1 mutations in chloroquine-resistant Plasmodium vivax isolates

March 3, 2020 - 12:31 -- Open Access
Spotin A, Mahami-Oskouei M, Ahmadpour E, Parsaei M, Rostami A, Emami S, Gholipour S, Farmani M
Transactions of The Royal Society of Tropical Medicine and Hygiene, traa002

Chloroquine (CQ) is generally prescribed as the front-line antimalarial drug of choice to treat Plasmodium vivax infections; however, some clinical CQ-resistant P. vivax isolates have been indigenously reported around the world during the last decade.

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