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antimalarial

Kitchen Sink Strategy and portfolio approach

August 17, 2018 - 14:09 -- William Jobin

It is valuable and refreshing to see contributions to strategies for malaria suppression in Africa from other disciplines, such as economics. Killeen and Reed pointed out that the portfolio effect cushions mosquito populations and malaria transmission against vector control interventions.(Killeen GF, Reed TE. Malar J. 2018 Aug 10;17(1):291. doi: 10.1186/s12936-018-2441-z.) Thus it must be considered when planning a strategy for Africa.

Not Open Access | Synthesis and antimalarial evaluation of a screening library based on a tetrahydroanthraquinone natural product scaffold

November 25, 2012 - 14:20 -- NOT Open Access
Author(s): 
Vanida Choomuenwai, Katherine T. Andrews, Rohan A. Davis
Reference: 
Bioorganic & Medicinal Chemistry, Volume 20, Issue 24, 15 December 2012, Pages 7167-7174
MalariaWorld

This compound displayed moderate cytotoxicity against neonatal foreskin fibroblast (NFF) cells with an IC50 of 15.6 μM.

Review: PfCRT and its role in antimalarial drug resistance

October 23, 2012 - 11:19 -- Patrick Sampao
Author(s): 
Andrea Ecker, Adele M. Lehane, Jérôme Clain, David A. Fidock
Reference: 
Trends in Parasitology, Volume 28, Issue 11, November 2012, Pages 504-514

MalariaWorldThese results highlight the need to be vigilant in screening for the appearance of novel pfcrt alleles that could contribute to new multi-drug resistance phenotypes.

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Not Open Access | In vitro and in vivo antimalarial evaluation of semi-synthetic derivatives of gomphostenin

June 29, 2012 - 14:09 -- Patrick Sampao
Author(s): 
Manisha Sathe, M.P. Kaushik
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 14, 15 July 2010, Pages 4233-4236

MalariaWorldGN derivatives 3 and 5 were found to have curative activity with moderate chemosuppression of 65% and 69%, respectively, at the dose level of 150 mg/kg/day.

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Antimalarial plant remedies from Burkina Faso: Their potential for prophylactic use

March 7, 2012 - 14:52 -- Patrick Sampao
Author(s): 
Rakiswendé Serge Yerbanga, Leonardo Lucantoni, Giulio Lupidi, Geme Urge Dori, Nzangue Roselyne Tepongning, Jean Baptiste Nikiéma, Fulvio Esposito, Annette Habluetzel
Reference: 
Journal of Ethnopharmacology, Volume 140, Issue 2, 27 March 2012, Pages 255-260

MalariaWorldThis study confirms, in the murine malaria system, the antiplasmodial properties of the examined remedies on the Plasmodium stages developing in the vertebrate host, thus encouraging studies aiming at identifying the active fractions and compounds responsible for the described activity and to develop standardized prophylactic remedies.

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Antimalarial evaluation and docking studies of hybrid phenylthiazolyl-1,3,5-triazine derivatives: A novel and potential antifolate lead for Pf-DHFR-TS inhibition

February 28, 2012 - 10:42 -- Patrick Sampao
Author(s): 
Prashant Gahtori, Surajit K. Ghosh, Pratap Parida, Anil Prakash, Kabita Gogoi, Hans Raj Bhat, Udaya Pratap Singh
Reference: 
Experimental Parasitology, Volume 130, Issue 3, March 2012, Pages 292-299

MalariaWorldFindings from the study disclose that a significant correlation was exist between in vitro results and in silico prediction (r2 = 0.543).

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2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites

March 9, 2011 - 08:21 -- Kabogo Ndegwa
Author(s): 
Swetlana, Heinrich Mirko, Altenkämper Benjamin, Bechem Johann, Perruchon Regina, Ortmann Hans-Martin, Dahse Yulin, Wang Michael, Lanzer Martin, Schlitzer
Reference: 
European Journal of Medicinal Chemistry, Volume 46, Issue 4, April 2011, Pages 1331-1342

Through the replacement of the 5-acylamino moiety by simple chlorine and further modifications of the 2-acylamino residue we could obtain inhibitors with improved selectivity towards malaria parasites combined with an acceptable reduction of antimalarial activity.

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Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines

September 6, 2010 - 09:29 -- Patrick Sampao
Author(s): 
Manolo Casagrande, Nicoletta Basilico, Chiara Rusconi, Donatella Taramelli, Anna Sparatore
Reference: 
Bioorganic & Medicinal Chemistry, Volume 18, Issue 18, 15 September 2010, Pages 6625-6633

The antimalarial activity of this new class of compounds seems to be related to the inhibition of heme detoxification process of parasites, as in the case of chloroquine.

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6-(4′-Aryloxy-phenyl)vinyl-1,2,4-trioxanes: A new series of orally active peroxides effective against multidrug-resistant Plasmodium yoelii in Swiss mice

July 15, 2010 - 09:52 -- Kabogo Ndegwa
Author(s): 
Chandan Singh, Ved Prakash Verma, Niraj Krishna Naikade, Ajit Shankar Singh, Mohammad Hassam, Sunil. K. Puri
Reference: 
Bioorganic & Medicinal Chemistry Letters Volume 20, Issue 15, 1 August 2010, Pages 4459-4463

A new series of 6-(4′-aryloxy-phenyl)vinyl-1,2,4-trioxanes 10a–d, 11a–d, and 12a–d have been synthesized and evaluated for their antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice by oral route.

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Rationale Design of Biotinylated Antimalarial Endoperoxide Carbon Centered Radical Prodrugs for Applications in Proteomics

May 25, 2010 - 09:12 -- Kabogo Ndegwa
Author(s): 
V Barton, SA Ward, J Chadwick, A Hill, PM O'Neill
Reference: 
J. Med. Chem, May 18, 2010

The semisynthetic artemisinin derivatives such as artesunate and artemether, along with the fully synthetic endoperoxide antimalarials (e.g., OZ277, Nature 2004, 430, 900−904), are believed to mediate their antimalarial effects by iron-induced formation of carbon-centered radicals capable of alkylating heme and/or protein.

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