We have identified a class of molecules, known as 2-aminothiazoles (2-ATs), as frequent-hitting
fragments in biophysical binding assays. This was exemplified by 4-phenylthiazol-2-…

Malaria is a devastating disease caused by Plasmodium parasites, resulting in approximately
435000 deaths in 2018. The impact of malaria is compounded by the emergence of …

TBPB and 77-LH-28-1 are selective agonists of the M 1 muscarinic acetylcholine receptor (mAChR)
that may gain their selectivity through a bitopic mechanism, interacting concomitantly …

A series of novel 2-amino-3-benzoylthiophenes (2A3BTs) were screened using a functional
assay of A 1 R mediated phosphorylation of extracellular signal-regulated kinases 1 and 2 (…

The conventional Richter cyclization involves diazotization of 2-alkynylanilines with HX (aq)
(X=Br or Cl) and NaNO 2 , followed by spontaneous ring closure to give a mixture of 4-…

The increasing incidence of antimalarial drug resistance to the first-line artemisinin combination
therapies underpins an urgent need for new antimalarial drugs, ideally with a novel …

New antimalarial compounds with novel mechanisms of action are urgently needed to combat
the recent rise in antimalarial drug resistance. Phenotypic high-throughput screens have …

The emergence of Plasmodium falciparum resistance to frontline antimalarials, including
artemisinin combination therapies, highlights the need for new molecules that act via novel …

The adenosine A 1 receptor (A 1 AR) is a potential novel therapeutic target for myocardial
ischemia-reperfusion injury. However, to date, clinical translation of prototypical A 1 AR …

Recent interest in the M 1 muscarinic acetylcholine (ACh) receptor (mAChR) has led to the
discovery of various selective agonists for the receptor. The novel selective agonist 1-(1′-(2-…