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Antimalarials

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Synthesis, identification and in vitro biological evaluation of some novel quinoline incorporated 1,3-thiazinan-4-one derivatives.

Bioorganic & medicinal chemistry letters
The present study describes the synthesis of two new series of 3-hydroxy-N-(4-oxo-2-phenyl-1,3-thiazinan-3-yl)-8-(trifluoromethyl)quinoline-2-carboxamide derivatives (4a-j) and 3-((7-chloroquinolin-4-ylamino)methyl)-2-phenyl-1,3-thiazinan-4-one deriv...

In silico prediction of anti-malarial hit molecules based on machine learning methods.

International journal of computational biology and drug design
Machine learning techniques have been widely used in drug discovery and development in the areas of cheminformatics. Aspartyl aminopeptidase (M18AAP) of Plasmodium falciparum is crucial for survival of malaria parasite. We have created predictive mod...

MALrisk: a machine-learning-based tool to predict imported malaria in returned travellers with fever.

Journal of travel medicine
BACKGROUND: Early diagnosis is key to reducing the morbi-mortality associated with P. falciparum malaria among international travellers. However, access to microbiological tests can be challenging for some healthcare settings. Artificial Intelligence...

IFPTML Mapping of Drug Graphs with Protein and Chromosome Structural Networks vs. Pre-Clinical Assay Information for Discovery of Antimalarial Compounds.

International journal of molecular sciences
The parasite species of genus causes Malaria, which remains a major global health problem due to parasite resistance to available Antimalarial drugs and increasing treatment costs. Consequently, computational prediction of new Antimalarial compounds...

Artificial Intelligence Applied to the Rapid Identification of New Antimalarial Candidates with Dual-Stage Activity.

ChemMedChem
Increasing reports of multidrug-resistant malaria parasites urge the discovery of new effective drugs with different chemical scaffolds. Protein kinases play a key role in many cellular processes such as signal transduction and cell division, making ...

Discovery of potential 1,3,5-Triazine compounds against strains of Plasmodium falciparum using supervised machine learning models.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
The Malaria burden was an escalating global encumbrance and need to be addressed with critical care. Anti-malarial drug discovery was integrated with supervised machine learning (ML) models to identify potent thiazolyl-traizine derivatives. This assi...

Machine learning analysis plans for randomised controlled trials: detecting treatment effect heterogeneity with strict control of type I error.

Trials
BACKGROUND: Retrospective exploratory analyses of randomised controlled trials (RCTs) seeking to identify treatment effect heterogeneity (TEH) are prone to bias and false positives. Yet the desire to learn all we can from exhaustive data measurements...

Deep Learning-driven research for drug discovery: Tackling Malaria.

PLoS computational biology
Malaria is an infectious disease that affects over 216 million people worldwide, killing over 445,000 patients annually. Due to the constant emergence of parasitic resistance to the current antimalarial drugs, the discovery of new drug candidates is ...

Development and rigorous validation of antimalarial predictive models using machine learning approaches.

SAR and QSAR in environmental research
The large collection of known and experimentally verified compounds from the ChEMBL database was used to build different classification models for predicting the antimalarial activity against . Four different machine learning methods, namely the supp...