'New/Designer Benzodiazepines': an analysis of the literature and psychonauts' trip reports

L Orsolini, JM Corkery, S Chiappini… - Current …, 2020 - ingentaconnect.com
Background: NPS belonging to the benzodiazepine (BZD) class, eg,'legal/designer
BZDs'/'research chemicals', have recently emerged in the drug (mainly online/virtual) market …

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains

O Mirguet, R Gosmini, J Toum… - Journal of medicinal …, 2013 - ACS Publications
The bromo and extra C-terminal domain (BET) family of bromodomains are involved in
binding epigenetic marks on histone proteins, more specifically acetylated lysine residues …

Respiratory syncytial virus infections: recent prospects for control

RW Sidwell, DL Barnard - Antiviral Research, 2006 - Elsevier
Respiratory syncytial virus (RSV) infections remain a significant public health problem
throughout the world, although recently developed and clinically approved anti-RSV …

RSV604, a novel inhibitor of respiratory syncytial virus replication

J Chapman, E Abbott, DG Alber… - Antimicrobial agents …, 2007 - Am Soc Microbiol
Respiratory syncytial virus (RSV) is the most common cause of lower respiratory tract
infections worldwide, yet no effective vaccine or antiviral treatment is available. Here we …

Toluene derivatives as simple coupling precursors for cascade palladium-catalyzed oxidative C–H bond acylation of acetanilides

Y Wu, PY Choy, F Mao, FY Kwong - Chemical Communications, 2013 - pubs.rsc.org
A palladium-catalyzed cascade cross-coupling of acetanilide and toluene for the synthesis
of ortho-acylacetanilide is described. Toluene derivatives can act as effective acyl …

Neuroprotective tri-and tetracyclic BChE inhibitors releasing reversible inhibitors upon carbamate transfer

FH Darras, B Kling, J Heilmann… - ACS Medicinal Chemistry …, 2012 - ACS Publications
Tri-and tetracyclic nitrogen-bridgehead compounds were designed and synthesized to yield
micromolar cholinesterase (ChE) inhibitors. Structure–activity relationships identified potent …

EDP-938, a novel nucleoprotein inhibitor of respiratory syncytial virus, demonstrates potent antiviral activities in vitro and in a non-human primate model

MHJ Rhodin, NV McAllister, J Castillo, SL Noton… - PLoS …, 2021 - journals.plos.org
EDP-938 is a novel non-fusion replication inhibitor of respiratory syncytial virus (RSV). It is
highly active against all RSV-A and B laboratory strains and clinical isolates tested in vitro in …

Transition‐Metal‐Free Decarboxylative Propargylic Substitution/Cyclization with either Azolium Enolates or Acyl Anions

S Lu, JY Ong, SB Poh, T Tsang, Y Zhao - Angewandte Chemie, 2018 - Wiley Online Library
Presented herein is an unprecedented transition‐metal‐free propargylic substitution
reaction with either azolium enolates or acyl anions, which are generated from aldehydes …

1, 4-Benzodiazepines as inhibitors of respiratory syncytial virus. The identification of a clinical candidate

EA Henderson, DG Alber, RC Baxter… - Journal of medicinal …, 2007 - ACS Publications
Respiratory syncytial virus (RSV) is the cause of one-fifth of all lower respiratory tract
infections worldwide and is increasingly being recognized as representing a serious threat …

New synthetic routes to triazolo-benzodiazepine analogues: expanding the scope of the bump-and-hole approach for selective bromo and extra-terminal (BET) …

MGJ Baud, E Lin-Shiao, M Zengerle… - Journal of medicinal …, 2016 - ACS Publications
We describe new synthetic routes developed toward a range of substituted analogues of
bromo and extra-terminal (BET) bromodomain inhibitors I-BET762/JQ1 based on the triazolo …