Molecular photoswitches in aqueous environments

J Volarić, W Szymanski, NA Simeth… - Chemical Society …, 2021 - pubs.rsc.org
Molecular photoswitches enable dynamic control of processes with high spatiotemporal
precision, using light as external stimulus, and hence are ideal tools for different research …

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery

B Das, ATK Baidya, AT Mathew, AK Yadav… - Bioorganic & Medicinal …, 2022 - Elsevier
Many lead compounds fail to reach clinical trials despite being potent because of low
bioavailability attributed to their insufficient solubility making solubility a primary and crucial …

Urea derivatives in modern drug discovery and medicinal chemistry

AK Ghosh, M Brindisi - Journal of medicinal chemistry, 2019 - ACS Publications
The urea functionality is inherent to numerous bioactive compounds, including a variety of
clinically approved therapies. Urea containing compounds are increasingly used in …

The necessary nitrogen atom: a versatile high-impact design element for multiparameter optimization

LD Pennington, DT Moustakas - Journal of Medicinal Chemistry, 2017 - ACS Publications
There is a continued desire in biomedical research to reduce the number and duration of
design cycles required to optimize lead compounds into high-quality chemical probes or …

[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 …

Targeting the pancreatic β-cell to treat diabetes

A Vetere, A Choudhary, SM Burns… - Nature reviews Drug …, 2014 - nature.com
Diabetes is a leading cause of morbidity and mortality worldwide, and predicted to affect
over 500 million people by 2030. However, this growing burden of disease has not been met …

Synthesis of medium-sized heterocycles by transition-metal-catalyzed intramolecular cyclization

M Choury, A Basilio Lopes, G Blond, M Gulea - Molecules, 2020 - mdpi.com
Medium-sized heterocycles (with 8 to 11 atoms) constitute important structural components
of several biologically active natural compounds and represent promising scaffolds in …

Application of fluorine-and nitrogen-walk approaches: defining the structural and functional diversity of 2-phenylindole class of cannabinoid 1 receptor positive …

S Garai, PM Kulkarni, PC Schaffer, LM Leo… - Journal of medicinal …, 2019 - ACS Publications
Cannabinoid 1 receptor (CB1R) allosteric ligands hold a far-reaching therapeutic promise.
We report the application of fluoro-and nitrogen-walk approaches to enhance the drug-like …

Ureas: applications in drug design

A Dhananjay Jagtap… - Current Medicinal …, 2017 - ingentaconnect.com
The unique hydrogen binding capabilities of ureas make them an important functional group
to make drug-target interactions and thus incorporated in small molecules displaying broad …

Conformational restriction and steric hindrance in medicinal chemistry

P Wipf, EM Skoda, A Mann - The practice of medicinal chemistry, 2015 - Elsevier
Conformational Restriction and Steric Hindrance in Medicinal Chemistry - ScienceDirect
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