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antimalarials

NOT Open Access | Fixed dose combinations of anti‐tubercular, antimalarial and antiretroviral medicines on the Indian market: critical analysis of ubiquity, sales and regulatory status

February 6, 2019 - 15:40 -- NOT Open Access
Author(s): 
Virendra S. Ligade, Tanmay M. Thakar, Swapnil J. Dengale
Reference: 
Tropical Medicine & International Health Volume24, Issue2 February 2019 Pages 238-246

A large proportion of FDC formulations available in India has never been approved by CDSCO, hence raising the doubts about their safety and efficacy.

NOT Open Access | Synthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybrids

October 2, 2018 - 16:46 -- NOT Open Access
Author(s): 
Christo de Lange, Dina Coertzen, Frans J. Smit, Johannes F. Wentzel, Ho Ning Wong, Lyn-Marie Birkholtz, Richard K. Haynes, David D. N'Da
Reference: 
Bioorganic & Medicinal Chemistry Letters Volume 28, Issue 19, 15 October 2018, Pages 3161-3163

Artemisinin-ferrocene conjugates incorporating a 1,2-disubstituted ferrocene analogous to that embedded in ferroquine but attached via a piperazine linker to C10 of the artemisinin were prepared from the piperazine artemisinin derivative, and activities were evaluated against asexual blood stages of chloroquine (CQ) sensitive NF54 and CQ resistant K1 and W2 strains of Plasmodium falciparum (Pf).

NOT Open Access | Artemisone and Artemiside Are Potent Panreactive Antimalarial Agents That Also Synergize Redox Imbalance in Plasmodium falciparum Transmissible Gametocyte Stages

August 1, 2018 - 14:39 -- NOT Open Access
Author(s): 
Dina Coertzen, Janette Reader, Richard K. Haynes, et al.
Reference: 
Antimicrob. Agents Chemother. August 2018 vol. 62 no. 8 e02214-17

The emergence of resistance toward artemisinin combination therapies (ACTs) by the malaria parasite Plasmodium falciparum has the potential to severely compromise malaria control.

How long do rapid diagnostic tests remain positive after anti-malarial treatment?

June 13, 2018 - 08:29 -- Open Access
Author(s): 
Ursula Dalrymple, Rohan Arambepola, Peter W. Gething and Ewan Cameron
Reference: 
Malaria Journal 2018 17:228, 8 June 2018

RDTs remain positive for a highly variable amount of time after treatment with anti-malarials, and the duration of positivity is highly dependent on the type of RDT used for diagnosis.

Medical Treatment: 

NOT Open Access | Synthesis and antimalarial evaluation of artesunate-polyamine and trioxolane-polyamine conjugates

October 30, 2017 - 06:15 -- NOT Open Access
Author(s): 
A. Norrie Pearce, Marcel Kaiser, Brent R. Copp
Reference: 
European Journal of Medicinal Chemistry Volume 140, 10 November 2017, Pages 595-603

A series of artesunate-polyamine and trioxolane-polyamine conjugates have been prepared.

NOT Open Access | 1,2,4-Triazole and 1,3,4-oxadiazole analogues: Synthesis, MO studies, in silico molecular docking studies, antimalarial as DHFR inhibitor and antimicrobial activities

July 12, 2017 - 16:23 -- NOT Open Access
Author(s): 
Sampark S. Thakkar, Parth Thakor, Hiren Doshi, Arabinda Ray
Reference: 
Bioorganic & Medicinal Chemistry, Volume 25, Issue 15, 1 August 2017, Pages 4064-4075

1,2,4-Triazole and 1,3,4-oxadiazole analogues are of interest due to their potential activity against microbial and malarial infections.

In vivo antiplasmodial activity and toxicological assessment of hydroethanolic crude extract of Ajuga remota

January 17, 2017 - 15:32 -- Open Access
Author(s): 
Aschalew Nardos and Eyasu Makonnen
Reference: 
Malaria Journal 2017 16:25, 13 January 2017

The investigation results suggest that the leave extract of Ajuga remota possesses antimalarial activity.

Analysis of anti-malarial resistance markers in pfmdr1 and pfcrt across Southeast Asia in the Tracking Resistance to Artemisinin Collaboration

November 10, 2016 - 17:39 -- Open Access
Author(s): 
Krongkan Srimuang, Olivo Miotto, Pharath Lim, Rick M. Fairhurst, Dominic P. Kwiatkowski, Charles J. Woodrow and Mallika Imwong
Reference: 
Malaria Journal 2016 15:541, 8 November 2016

These findings generate cause for concern regarding the mid-term efficacy of artemether–lumefantrine in Myanmar, while the absence of resistance-conferring pfmdr1 mutations and SVMNT pfcrt haplotypes suggests that amodiaquine could be an efficacious component of anti-malarial regimens in SEA.

Medical Treatment: 

NOT Open Access | Design, synthesis and antimalarial evaluation of novel thiazole derivatives

August 8, 2016 - 10:06 -- NOT Open Access
Author(s): 
José María Bueno, Miguel Carda, Benigno Crespo, Ana Carmen Cuñat, Cristina de Cozar, María Luisa León, J. Alberto Marco, Nuria Roda, Juan F. Sanz-Cervera
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 26, Issue 16, 15 August 2016, Pages 3938–3944

As part of our medicinal chemistry program’s ongoing search for compounds with antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study analyzing their in vitro activities against the chloroquine-sensitive Plasmodium falciparum 3D7 strain.

Medical Condition: 

NOT Open Access | Bistacrine derivatives as new potent antimalarials

July 23, 2016 - 17:59 -- NOT Open Access
Author(s): 
Ines Schmidt, Gabriele Pradel, Ludmilla Sologub, Alexandra Golzmann, Che J. Ngwa, Anna Kucharski, Tanja Schirmeister, Ulrike Holzgrabe
Reference: 
Bioorganic & Medicinal Chemistry, Volume 24, Issue 16, 15 August 2016, Pages 3636–3642

Linking two tacrine molecules results in a tremendous increase of activity against Plasmodia in comparison to the monomer.

Medical Treatment: 

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