New developments in anti-malarial target candidate and product profiles
JN Burrows, S Duparc, WE Gutteridge… - Malaria journal, 2017 - Springer
A decade of discovery and development of new anti-malarial medicines has led to a
renewed focus on malaria elimination and eradication. Changes in the way new anti …
renewed focus on malaria elimination and eradication. Changes in the way new anti …
Advances in high‐throughput mass spectrometry in drug discovery
High‐throughput (HT) screening drug discovery, during which thousands or millions of
compounds are screened, remains the key methodology for identifying active chemical …
compounds are screened, remains the key methodology for identifying active chemical …
[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology
CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …
probes of disease-related targets and potential starting points for drug discovery. In this …
Strategies for the diversity-oriented synthesis of macrocycles
Macrocycles have long been recognized as useful chemical entities for medicine, with
naturally occurring and synthetic macrocycles clinically approved for use as prescription …
naturally occurring and synthetic macrocycles clinically approved for use as prescription …
Diversity-oriented synthesis yields novel multistage antimalarial inhibitors
N Kato, E Comer, T Sakata-Kato, A Sharma, M Sharma… - Nature, 2016 - nature.com
Antimalarial drugs have thus far been chiefly derived from two sources—natural products
and synthetic drug-like compounds. Here we investigate whether antimalarial agents with …
and synthetic drug-like compounds. Here we investigate whether antimalarial agents with …
[HTML][HTML] Recent advances in malaria drug discovery
MA Biamonte, J Wanner, KG Le Roch - Bioorganic & medicinal chemistry …, 2013 - Elsevier
This digest covers some of the most relevant progress in malaria drug discovery published
between 2010 and 2012. There is an urgent need to develop new antimalarial drugs. Such …
between 2010 and 2012. There is an urgent need to develop new antimalarial drugs. Such …
Advancing biological understanding and therapeutics discovery with small-molecule probes
Small-molecule probes can illuminate biological processes and aid in the assessment of
emerging therapeutic targets by perturbing biological systems in a manner distinct from …
emerging therapeutic targets by perturbing biological systems in a manner distinct from …
The development process for discovery and clinical advancement of modern antimalarials
Malaria is a devastating disease caused by Plasmodium parasites, resulting in
approximately 435000 deaths in 2018. The impact of malaria is compounded by the …
approximately 435000 deaths in 2018. The impact of malaria is compounded by the …
Diversity-oriented synthesis as a tool for identifying new modulators of mitosis
BM Ibbeson, L Laraia, E Alza, CJ O'Connor… - Nature …, 2014 - nature.com
The synthesis of diverse three-dimensional libraries has become of paramount importance
for obtaining better leads for drug discovery. Such libraries are predicted to fare better than …
for obtaining better leads for drug discovery. Such libraries are predicted to fare better than …
Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit P. falciparum Dihydroorotate Dehydrogenase
Dihydroorotate dehydrogenase (DHODH) is an enzyme necessary for pyrimidine
biosynthesis in protozoan parasites of the genus Plasmodium, the causative agents of …
biosynthesis in protozoan parasites of the genus Plasmodium, the causative agents of …