Unpacking the Pathogen Box—an open source tool for fighting neglected tropical disease

CGL Veale - ChemMedChem, 2019 - Wiley Online Library
Abstract The Pathogen Box is a 400‐strong collection of drug‐like compounds, selected for
their potential against several of the world's most important neglected tropical diseases …

Imidazo [1, 2-b] pyridazine as privileged scaffold in medicinal chemistry: an extensive review

A Garrido, G Vera, PO Delaye… - European Journal of …, 2021 - Elsevier
Abstract Imidazo [1, 2-b] pyridazine scaffold represents an important class of heterocyclic
nucleus which provides various bioactives molecules. Among them, the successful kinase …

Identification of a potential antimalarial drug candidate from a series of 2-aminopyrazines by optimization of aqueous solubility and potency across the parasite life …

C Le Manach, AT Nchinda, T Paquet… - Journal of medicinal …, 2016 - ACS Publications
Introduction of water-solubilizing groups on the 5-phenyl ring of a 2-aminopyrazine series
led to the identification of highly potent compounds against the blood life-cycle stage of the …

Structural Basis for Inhibitor Potency and Selectivity of Plasmodium falciparum Phosphatidylinositol 4-Kinase Inhibitors

S Fienberg, CJ Eyermann, LB Arendse… - ACS Infectious …, 2020 - ACS Publications
Plasmodium falciparum phosphatidylinositol 4-kinase (Pf PI4K) has emerged as a promising
new drug target for novel antimalarial therapeutics. In the absence of a reliable high …

Copper(II)-Mediated Aerobic Synthesis of Imidazo[1,2-a]pyridines via Cascade Aminomethylation/Cycloisomerization of Alkynes

IV Rassokhina, VZ Shirinian, IV Zavarzin… - The journal of organic …, 2015 - ACS Publications
A single copper (II)-catalyzed three-component cascade aminomethylation/
cycloisomerization of propiolates to form imidazo [1, 2-a] pyridines was explored. A …

Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4 …

A Vallone, S D'Alessandro, S Brogi, M Brindisi… - European journal of …, 2018 - Elsevier
Therapies addressing multiple stages of Plasmodium falciparum life cycle are highly
desirable for implementing malaria elimination strategies. MMV019918 (1, 1-[5-(4-bromo-2 …

Reliable Functionalization of 5, 6‐Fused Bicyclic N‐Heterocycles Pyrazolopyrimidines and Imidazopyridazines via Zinc and Magnesium Organometallics

S Kumar Rout, A Kastrati, H Jangra… - … A European Journal, 2022 - Wiley Online Library
DFT‐calculations allow prediction of the reactivity of uncommon N‐heterocyclic scaffolds of
pyrazolo [1, 5‐a] pyrimidines and imidazo [1, 2‐b] pyridazines and considerably facilitate …

Insights into integrated lead generation and target identification in malaria and tuberculosis drug discovery

J Okombo, K Chibale - Accounts of Chemical Research, 2017 - ACS Publications
Conspectus New, safe and effective drugs are urgently needed to treat and control malaria
and tuberculosis, which affect millions of people annually. However, financial return on …

Selective inhibitors of Plasmodium falciparum glycogen synthase-3 (PfGSK-3): New antimalarial agents?

A Masch, C Kunick - Biochimica et Biophysica Acta (BBA)-Proteins and …, 2015 - Elsevier
Plasmodium falciparum glycogen synthase kinase-3 (PfGSK-3) is one of the eukaryotic
protein kinases that were identified as essential for the parasite causing malaria tropica …

Alkynoates as versatile and powerful chemical tools for the rapid assembly of diverse heterocycles under transition-metal catalysis: recent developments and …

I Khan, A Ibrar, S Zaib - Topics in Current Chemistry, 2021 - Springer
Heterocycles, heteroaromatics and spirocyclic entities are ubiquitous components of a wide
plethora of synthetic drugs, biologically active natural products, marketed pharmaceuticals …