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antimalarial

Antimalarial compounds from the aerial parts of Flacourtia indica (Flacourtiaceae)

July 21, 2010 - 09:03 -- Patrick Sampao
Author(s): 
Ali M., Valérie M., et al.
Reference: 
Journal of Ethnopharmacology, Volume 130, Issue 2, 20 July 2010, Pages 272-274

This study reports for the first time antiplasmodial activity for Flacourtia indica, for its AcOEt extract and the three major constituents and confirms its traditional use.

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Antimalarial 3-arylamino-6-benzylamino-1,2,4,5-tetrazines

July 16, 2010 - 08:00 -- Kabogo Ndegwa
Author(s): 
Duong Nhu, Sandra Duffy, Vicky M. Avery, Andrew Hughes, Jonathan B. Baell
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 15, 1 August 2010, Pages 4496-4498

We report on novel 3-arylamino-6-benzylamino-1,2,4,5-tetrazines with potent activity against Plasmodium falciparum.

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New antimalarials with a triterpenic scaffold from Momordica balsamina

July 13, 2010 - 06:53 -- Kabogo Ndegwa
Author(s): 
Cátia Ramalhete, Dinora Lopes, Silva Mulhovo, Joseph Molnár, Virgílio E. Rosário, Maria-José U. Ferreira
Reference: 
Bioorganic & Medicinal Chemistry, Volume 18, Issue 14, 15 July 2010, Pages 5254-5260

Bioassay-guided fractionation of the methanol extract of Momordica balsamina led to the isolation of three new cucurbitane-type triterpenoids, balsaminols C–E (1–3). Their structures were elucidated on the basis of spectroscopic methods including 2D NMR experiments (COSY, HMQC, HMBC and NOESY).

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Open Access | Evaluation of the potential of the marine sponges of the Zanzibar Island to yield antimalarial and antimicrobial active compounds

July 7, 2010 - 08:59 -- Kabogo Ndegwa
Author(s): 
S. A. Said, M. J. Moshi, R. S.O. Nondo, P. J. Masimba, E. Innocent, A. Guantai
Reference: 
Tanzania Journal of Health Research, Vol 12, No 3 (2010)

These results support the need for intensified efforts to search for active antimalarial and antimicrobial compounds from the Zanzibar marine sponges.

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Inflamation: Heme Impairs Prostaglandin E2 and TGF-β Production by Human Mononuclear Cells via Cu/Zn Superoxide Dismutase: Insight into the Pathogenesis of Severe Malaria

July 6, 2010 - 06:38 -- Kabogo Ndegwa
Author(s): 
Bruno B. Andrade, Théo Araújo-Santos, Nívea F. Luz, Ricardo Khouri, Marcelo T. Bozza, Luís M. A. Camargo, Aldina Barral, Valéria M. Borges, and Manoel Barral-Netto
Reference: 
The Journal of Immunology, 2010, 185, 1196 -1204

In many hemolytic disorders, such as malaria, the release of free heme has been involved in the triggering of oxidative stress and tissue damage. Patients presenting with severe forms of malaria commonly have impaired regulatory responses.

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In vitro and in vivo antimalarial evaluation of semi-synthetic derivatives of gomphostenin

June 29, 2010 - 11:56 -- Kabogo Ndegwa
Author(s): 
Manisha Sathe, M.P. Kaushik
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 14, 15 July 2010, Pages 4233-4236

A novel series of semi-synthetic gomphostenin derivatives (1–9) were prepared utilizing C-14 hydroxyl group for the first time and studied for their antimalarial properties.

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In vivo antimalarial evaluation of Gomphostenins

June 23, 2010 - 12:20 -- Patrick Sampao
Author(s): 
M. Sathe, R. Ghorpade, A.K. Srivastava, M.P. Kaushik
Reference: 
Journal of Ethnopharmacology, Volume 130, Issue 1, 6 July 2010, Pages 171-174

The studies have indicated that clerodane class of diterpenes GN–6 and GN–10 certainly holds great promise for malaria control and will be useful in antimalarial chemotherapy.

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Invited Review: Quinolines and structurally related heterocycles as antimalarials

June 14, 2010 - 12:53 -- Kabogo Ndegwa
Author(s): 
Kirandeep Kaur, Meenakshi Jain, Ravi P. Reddy, Rahul Jain
Reference: 
European Journal of Medicinal Chemistry, Volume 45, Issue 8, August 2010, Pages 3245-3264

The quinoline scaffold is prevalent in a variety of pharmacologically active synthetic and natural compounds. The discovery of chloroquine, the most famous drug containing this scaffold resulted in control and eradication of malaria for decades. The other known antimalarial drugs from the quinoline family include: quinine, amodiaquine, piperaquine, primaquine, and mefloquine.

Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline

June 14, 2010 - 12:48 -- Kabogo Ndegwa
Author(s): 
Anna Sparatore, Nicoletta Basilico, Manolo Casagrande, Silvia Parapini, Donatella Taramelli, Reto Brun, Sergio Wittlin, Fabio Sparatore
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 18, Issue 13, 1 July 2008, Pages 3737-3740

Two pyrrolizidinylalkyl derivatives of 4-amino-7-chloroquinoline (MG2 and MG3) were prepared and tested in vitro against CQ-sensitive and CQ-resistant strains of Plasmodium falciparum and in vivo in a Plasmodium berghei mouse model of infection.

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Synthesis and antiplasmodial activity of lycorine derivatives

June 14, 2010 - 12:39 -- Kabogo Ndegwa
Author(s): 
Juan C. Cedrón, David Gutiérrez, Ninoska Flores, Ángel G. Ravelo, Ana Estévez-Braun
Reference: 
Bioorganic & Medicinal Chemistry, Volume 18, Issue 13, 1 July 2010, Pages 4694-4701

Twenty seven lycorine derivatives were prepared and evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum.

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