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1. Bed Nets, Insecticides, and Antimalarials: Where to Next?

Author:
Buchanan, Hayley D.; McFadden, Geoffrey I.; Goodman, Christopher D.
Source:
Trends in parasitology 2019 v.35 no.9 pp. 668-670
ISSN:
1471-4922
Subject:
antimalarials,   etc   ; Culicidae; bed nets; insecticide resistance; insecticides; malaria; parasites;     Show all 7 Subjects
Abstract:
... Insecticide-impregnated bed nets have saved millions from fatal malaria, but their effectiveness is waning due to mosquito insecticide resistance. A new strategy (Paton et al., Nature, 2019) to deliver parasiticidal compounds into mosquitoes to kill transmission-stage parasites could enhance the effectiveness of bed nets and get around the perennial problems of resistance. ...
DOI:
10.1016/j.pt.2019.06.009

2. First enantioselective synthesis of salinipostin A, a marine cyclic enol-phosphotriester isolated from Salinispora sp

Author:
Okamura, Hironori; Fujioka, Takanobu; Mori, Naoki; Taniguchi, Tohru; Monde, Kenji; Watanabe, Hidenori; Takikawa, Hirosato
Source:
Tetrahedron letters 2019 pp. 150917
ISSN:
0040-4039
Subject:
antimalarials,   etc   ; chemical reactions; chemical structure; enantioselective synthesis; organic compounds; regioselectivity;     Show all 6 Subjects
Abstract:
... Salinipostins are cyclic enol-phosphotriesters isolated from a marine-derived Salinispora sp. as antimalarial compounds. Herein, the first enantioselective synthesis of salinipostin A was achieved. Organocatalyst-mediated asymmetric cyclopropanation and regioselective cyclopropane ring opening were the key steps. ...
DOI:
10.1016/j.tetlet.2019.07.008

3. A review of the applications of Schiff bases as optical chemical sensors

Author:
Berhanu, Asnake Lealem; Gaurav,; Mohiuddin, Irshad; Malik, Ashok Kumar; Aulakh, Jatinder Singh; Kumar, Vanish; Kim, Ki-Hyun
Source:
Trends in analytical chemistry 2019 v.116 pp. 74-91
ISSN:
0165-9936
Subject:
antimalarials,   etc   ; anions; cations; chemical species; fluorescence; metals; schiff bases; toxicity;     Show all 8 Subjects
Abstract:
... Schiff bases and their metal complexes have become well-known for catalytic (e.g., in various synthetic processes) and biological properties (e.g., antifungal, antibacterial, anti-malarial, and antiviral characteristics) since their discovery by Hugo Schiff in 1864. As synthetic compounds, they are employed as versatile tools in numerous applications such as fluorescent turn-on/turn-off sensors fo ...
DOI:
10.1016/j.trac.2019.04.025

4. Total synthesis and antimalarial activity of mortiamides A–D

Author:
Bérubé, Christopher; Gagnon, Dominic; Borgia, Alexandre; Richard, Dave; Voyer, Normand
Source:
Chemical communications 2019 v.55 no.52 pp. 7434-7437
ISSN:
1364-548X
Subject:
antimalarials,   etc   ; Mortierella; antiplasmodial properties; chemical compounds; marine sediments; oligomerization; Canada;     Show all 7 Subjects
Abstract:
... Mortiamides A–D (1–4) are head-to-tail cyclic heptapeptides that were identified from a novel Mortierella sp. isolate obtained from marine sediments from Northern Canada. Herein we report the first total synthesis of mortiamides A–D (1–4) on a solid support by concomitant cyclization/cleavage without any oligomerization side reactions, and overall yields up to 48%. We also report on the antiplasmo ...
DOI:
10.1039/c9cc02864a

5. para-Aminobenzoate Synthesis versus Salvage in Malaria Parasites

Author:
Mather, Michael W.; Ke, Hangjun
Source:
Trends in parasitology 2019 v.35 no.3 pp. 176-178
ISSN:
1471-4922
Subject:
antimalarials,   etc   ; diet; enzymes; folic acid; malaria; mice; models; parasites;     Show all 8 Subjects
Abstract:
... Enzymes of the folate de novo synthesis pathway in malaria parasites are proven antimalarial drug targets. A key precursor for folate synthesis is para-aminobenzoate (pABA). In a recent study [1] (Cell Rep. 2019;26:356–363 e4), the contributions of pABA synthesis versus salvage were re-evaluated in a rodent malaria model with knockout parasites grown in mice fed with various diets. The results imp ...
DOI:
10.1016/j.pt.2019.01.010

6. Synthesis, Antimalarial Activity, and Docking Studies of Monocarbonyl Analogues of Curcumin

Author:
Yusuf, Amina S.; Sada, Ibrahim; Hassan, Yusuf; Olomola, Temitope O.; Adeyemi, Christiana M.; Ajibade, Sunday O.
Source:
Analele Universității "Ovidius" Constanța 2018 v.29 no.2 pp. 92-96
ISSN:
2286-038X
Subject:
antimalarials,   etc   ; bioactive properties; computer simulation; curcumin; parasites;     Show all 5 Subjects
Abstract:
... The synthesis of five monocarbonyl analogues of curcumin is described. In vitro anti-malarial assay of the compounds was carried out and the effect of the substituents on the aryl ring has been described. The results show that all the five compounds exhibited some reasonable activity against the chloroquine-resistant plasmodium parasite. Molecular docking studies further confirmed the observed bio ...
DOI:
10.2478/auoc-2018-0013

7. Targeting Plasmodium Proteases to Block Malaria Parasite Escape and Entry

Author:
Paul, Aditya S.; Duraisingh, Manoj T.
Source:
Trends in parasitology 2018 v.34 no.2 pp. 95-97
ISSN:
1471-4922
Subject:
antimalarials,   etc   ; Plasmodium; erythrocytes; malaria; parasites; plasmepsin;     Show all 6 Subjects
Abstract:
... Proliferation of malaria parasites in a host requires mechanisms to spread between red blood cells (RBCs). We discuss here the implications for biology and antimalarial drug development of companion studies that establish the requirement of two Plasmodium spp. proteases of the plasmepsin family in parasite egress from, and invasion into, RBCs. ...
DOI:
10.1016/j.pt.2017.11.012

8. LC–MS/MS quantitation of antimalarial drug piperaquine and metabolites in human plasma B Analytical technologies in the biomedical and life sciences

Author:
Aziz, Mohd Yusmaidie; Hoffmann, Kurt-Jürgen; Ashton, Michael
Source:
Journal of chromatography 2017 v.1063 pp. 253-258
ISSN:
1570-0232
Subject:
antimalarials,   etc   ; chromatography; humans; metabolites; piperaquine;     Show all 5 Subjects
Abstract:
... This study aimed to develop a sensitive, quantitative assay for the antimalarial piperaquine (PQ) and its metabolites M1 and M2 in human plasma.Analytes were gradiently separated on a C18 column and detected with a Sciex API 4000 MS/MS with an ESI source operated in the positive ion mode with deuterated PQ as internal standard. The response was linear in the range 3.9–2508nM with a runtime of 7.0m ...
DOI:
10.1016/j.jchromb.2017.06.035

9. Introduction to the Special Issue on Malaria

Author:
Tuteja, Renu
Source:
The FEBS journal 2017 v.284 no.16 pp. 2550-2552
ISSN:
1742-464X
Subject:
antimalarials,   etc   ; drug resistance; malaria; vaccines;     Show all 4 Subjects
Abstract:
... This minireview series highlights recent developments in malaria research. The reviews cover diverse topics, from conventional antimalarial therapies and the strategies used to circumvent the emergence of drug resistance, to the latest approaches for the discovery and validation of new druggable targets and for the development of effective antimalarial vaccines. ...
DOI:
10.1111/febs.14128

10. Curcumin-nicotinamide cocrystallization with supercritical solvent (CSS): Synthesis, characterization and in vivo antinociceptive and anti-inflammatory activities

Author:
Ribas, Marcela M.; Aguiar, Gean Pablo S.; Muller, Liz G.; Siebel, Anna M.; Lanza, Marcelo; Oliveira, J. Vladimir
Source:
Industrial crops and products 2019 v.139 pp. 111537
ISSN:
0926-6690
Subject:
antimalarials,   etc   ; active pharmaceutical ingredients; anti-inflammatory activity; antioxidant activity; bioavailability; curcumin; pharmaceutical industry; polyphenols; solubility; solvents;     Show all 10 Subjects
Abstract:
... Curcumin is a bioactive polyphenol, which presents several medicinal benefits such as antinociceptive, anti-inflammatory, anti-carcinogenic, antimalarial, and antioxidant activity. Despite the benefits, the main barrier in curcumin use by pharmaceutical industry is its low solubility in water medium and hence low bioavailability. The cocrystallization process is characterized by the incidence of m ...
DOI:
10.1016/j.indcrop.2019.111537

11. Copper–Hydride-Catalyzed Enantioselective Processes with Allenyl Boronates. Mechanistic Nuances, Scope, and Utility in Target-Oriented Synthesis

Author:
Sun, Yu; Zhou, Yuebiao; Shi, Ying; del Pozo, Juan; Torker, Sebastian; Hoveyda, Amir H.
Source:
Journal of the American Chemical Society 2019 v.141 no.30 pp. 12087-12099
ISSN:
1520-5126
Subject:
antimalarials,   etc   ; alkynes; bioactive compounds; catalytic activity; diastereoselectivity; enantioselective synthesis; enantioselectivity; hydrides; phosphates;     Show all 9 Subjects
Abstract:
... Synthesis of complex bioactive molecules is substantially facilitated by transformations that efficiently and stereoselectively generate polyfunctional compounds. Designing such processes is hardly straightforward, however, especially when the desired route runs counter to the inherently favored reactivity profiles. Furthermore, in addition to being efficient and stereoselective, it is crucial tha ...
DOI:
10.1021/jacs.9b05465

12. Total Synthesis of the Antimalarial Ascidian Natural Product Albopunctatone

Author:
Pullella, Glenn A.; Wdowiak, Adam P.; Sykes, Melissa L.; Lucantoni, Leonardo; Sukhoverkov, Kirill V.; Zulfiqar, Bilal; Sobolev, Alexandre N.; West, Nicholas P.; Mylne, Joshua S.; Avery, Vicky M.; Piggott, Matthew J.
Source:
Organic letters 2019 v.21 no.14 pp. 5519-5523
ISSN:
1523-7052
Subject:
antimalarials,   etc   ; Lewis bases; Plasmodium falciparum; anthraquinones; chemical reactions; chemical structure; mammals; pathogens; regioselectivity; toxicity;     Show all 10 Subjects
Abstract:
... The first approaches to the 10′-anthronyl-2-anthraquinone skeleton have been devised, allowing two syntheses of the marine natural product albopunctatone. Both routes involve regioselective addition of a nucleophilic masked anthraquinone to a protected chrysazin derivative; the best affords albopunctatone in five steps and 35% overall yield. Albopunctatone exhibits potent inhibitory activity again ...
DOI:
10.1021/acs.orglett.9b01838

13. Nano-facilitated drug delivery strategies in the treatment of plasmodium infection

Author:
Puttappa, Nethravathi; Kumar, Raman Suresh; Kuppusamy, Gowthamarajan; Radhakrishnan, Arun
Source:
Acta tropica 2019 v.195 pp. 103-114
ISSN:
0001-706X
Subject:
antimalarials,   etc   ; drug therapy; drug toxicity; financial economics; malaria; morbidity; mortality; multiple drug resistance; nanocarriers; pharmacokinetics; vaccines;     Show all 11 Subjects
Abstract:
... Malaria, one of the major infectious disease-causing sizeable morbidity, mortality and economic loss worldwide. The main drawback for the failure to eradicate malaria is the spread of multiple drug resistance to the majority of currently available chemotherapy. At present nanotechnology offers an advanced opportunity in the delivery of drugs and vaccines to the desired targeted site in the body fo ...
DOI:
10.1016/j.actatropica.2019.04.020

14. Comparison of hyperspectral imaging techniques for the elucidation of falsified medicines composition

Author:
Coic, Laureen; Sacré, Pierre-Yves; Dispas, Amandine; Sakira, Abdoul Karim; Fillet, Marianne; Marini, Roland D.; Hubert, Philippe; Ziemons, Eric
Source:
Talanta 2019 v.198 pp. 457-463
ISSN:
0039-9140
Subject:
antimalarials,   etc   ; Fourier transform infrared spectroscopy; drugs; hyperspectral imagery; inorganic compounds; microscopy; organic compounds;     Show all 7 Subjects
Abstract:
... Hyperspectral imaging has shown a high potential to analyze falsifications of solid pharmaceutical products since the last decade. Thanks to the non-destructive, ecological and non-invasive properties, it is a preferred technique for these kinds of applications. Moreover, thanks to the spectroscopic properties, it is possible to detect as well organic compounds as inorganic compounds in a single a ...
DOI:
10.1016/j.talanta.2019.02.032

15. Novel Approaches to Control Malaria in Forested Areas of Southeast Asia

Author:
von Seidlein, Lorenz; Peto, Thomas J.; Tripura, Rupam; Pell, Christopher; Yeung, Shunmay; Kindermans, Jean Marie; Dondorp, Arjen; Maude, Richard
Source:
Trends in parasitology 2019 v.35 no.6 pp. 388-398
ISSN:
1471-4922
Subject:
antimalarials,   etc   ; bed nets; chemoprevention; drug resistance; foresters; forests; insecticides; malaria; South East Asia;     Show all 9 Subjects
Abstract:
... The emergence and spread of drug resistance in the Greater Mekong Subregion (GMS) have added urgency to accelerate malaria elimination while reducing the treatment options. The remaining foci of malaria transmission are often in forests, where vectors tend to bite during daytime and outdoors, thus reducing the effectiveness of insecticide-treated bed nets. Limited periods of exposure suggest that ...
DOI:
10.1016/j.pt.2019.03.011

16. Visible-Light-Photocatalyzed Reductions of N-Heterocyclic Nitroaryls to Anilines Utilizing Ascorbic Acid Reductant

Author:
Todorov, Aleksandar R.; Aikonen, Santeri; Muuronen, Mikko; Helaja, Juho
Source:
Organic letters 2019 v.21 no.10 pp. 3764-3768
ISSN:
1523-7052
Subject:
antimalarials,   etc   ; aminoquinolines; ascorbic acid; blue light; chemical structure; electron transfer; photocatalysts; reducing agents;     Show all 8 Subjects
Abstract:
... A photoreductive protocol utilizing [Ru(bpy)₃]²⁺ photocatalyst, blue light LEDs, and ascorbic acid (AscH₂) has been developed to reduce nitro N-heteroaryls to the corresponding anilines. Based on experimental and computational results and previous studies, we propose that the reaction proceeds via proton-coupled electron transfer between AscH₂, photocatalyst, and the nitro N-heteroaryl. The method ...
DOI:
10.1021/acs.orglett.9b01205

17. Enantioselective Total Synthesis of (+)-Monocerin, a Dihydroisocoumarin Derivative with Potent Antimalarial Properties

Author:
Ghosh, Arun K.; Lee, Daniel S.
Source:
Journal of organic chemistry 2019 v.84 no.10 pp. 6191-6198
ISSN:
1520-6904
Subject:
antimalarials,   etc   ; Lewis acids; acetates; diastereoselectivity; dihydroxylation; enantioselective synthesis; enantioselectivity; isocoumarins; moieties; organic chemistry; oxidation;     Show all 11 Subjects
Abstract:
... We describe here the enantioselective synthesis of (+)-monocerin and its acetate derivative. The present synthesis features an efficient optically active synthesis of the β-hydroxy-γ-lactone derivative with high enantiomeric purity using Sharpless dihydroxylation as the key step. The synthesis also highlights a tandem Lewis acid-catalyzed, oxocarbenium ion-mediated diastereoselective syn-allylatio ...
DOI:
10.1021/acs.joc.9b00414

18. Diversity of natural products of the genera Curvularia and Bipolaris

Author:
Khiralla, Afra; Spina, Rosella; Saliba, Sahar; Laurain-Mattar, Dominique
Source:
Fungal biology reviews 2019 v.33 no.2 pp. 101-122
ISSN:
1749-4613
Subject:
antimalarials,   etc   ; Anthozoa; Bipolaris; Curvularia; antioxidants; chemical structure; endophytes; fish; phytotoxicity; secondary metabolites; virulent strains;     Show all 11 Subjects
Abstract:
... Covering from 1963 to 2017.This review provides a summary of some secondary metabolites isolated from the genera Curvularia and Bipolaris from 1963 to 2017. The study has a broad objective. First to afford an overview of the structural diversity of these genera, classifying them depending on their chemical classes, highlighting individual examples of chemical structures. Also some information rega ...
DOI:
10.1016/j.fbr.2018.09.002

19. Gametocyte Sex Ratio: The Key to Understanding Plasmodium falciparum Transmission?

Author:
Tadesse, Fitsum G.; Meerstein-Kessel, Lisette; Gonçalves, Bronner P.; Drakeley, Chris; Ranford-Cartwright, Lisa; Bousema, Teun
Source:
Trends in parasitology 2019 v.35 no.3 pp. 226-238
ISSN:
1471-4922
Subject:
antimalarials,   etc   ; Culicidae; Plasmodium falciparum; diagnostic techniques; females; gametocytes; malaria; males; parasites; sex ratio; transcriptomics;     Show all 11 Subjects
Abstract:
... A mosquito needs to ingest at least one male and one female gametocyte to become infected with malaria. The sex of Plasmodium falciparum gametocytes can be determined microscopically but recent transcriptomics studies paved the way for the development of molecular methods that allow sex-ratio assessments at much lower gametocyte densities. These sex-specific gametocyte diagnostics were recently us ...
DOI:
10.1016/j.pt.2018.12.001

20. Antiplasmodial prenylated flavonoids from stem bark of Erythrina latissima

Author:
Tuenter, Emmy; Zarev, Yancho; Matheeussen, An; Elgorashi, Esameldin; Pieters, Luc; Foubert, Kenn
Source:
Phytochemistry letters 2019
ISSN:
1874-3900
Subject:
antimalarials,   etc   ; Erythrina; Plasmodium falciparum; antiplasmodial properties; bark; cytotoxicity; flavonoids; inhibitory concentration 50; stems; South Africa;     Show all 10 Subjects
Abstract:
... The antiplasmodial activity against Plasmodium falciparum strain K1 as well as cytotoxicity against MRC-5 cells of 15 prenylated flavonoids obtained from Erythrina latissima E. Mey (Leguminosae) from South Africa was determined. Although initially some promising activities were observed, with 5’-prenyl-pratensein being the most selective compound, most IC50 values varied from 1 to 30 µM, with cyto ...
DOI:
10.1016/j.phytol.2019.02.001