New and unusual scaffolds in medicinal chemistry

CM Marson - Chemical Society Reviews, 2011 - pubs.rsc.org
Contemporary medicinal chemistry faces diverse challenges from several directions,
including the need for both potency and specificity of any therapeutic agent; the increasingly …

Catalytic asymmetric construction of spiropyrrolidines via 1, 3-dipolar cycloaddition of azomethine ylides

X Fang, CJ Wang - Organic & Biomolecular Chemistry, 2018 - pubs.rsc.org
Spirocyclic pyrrolidines are structural motifs frequently found in a wide variety of natural
products, pharmaceuticals and biologically significant compounds. In the past few years …

Catalyst-free organic transformations under visible-light

M Tavakolian, M Hosseini-Sarvari - ACS Sustainable Chemistry & …, 2021 - ACS Publications
Pollutants from industry and chemical laboratories have harmful effects on human health
and the environment. Concerns about this problem have led to the development of more …

Improving drug design: an update on recent applications of efficiency metrics, strategies for replacing problematic elements, and compounds in nontraditional drug …

NA Meanwell - Chemical Research in Toxicology, 2016 - ACS Publications
Drug discovery and development is a complex and lengthy enterprise that suffers from high
rates of candidate attrition at all stages of the process. The physical, biological, and …

Recent advances of chroman-4-one derivatives: synthetic approaches and bioactivities

S Emami, Z Ghanbarimasir - European Journal of Medicinal Chemistry, 2015 - Elsevier
Chroman-4-one scaffold is a privileged structure in heterocyclic chemistry and drug
discovery. Also, chroman-4-ones are important intermediates and interesting building blocks …

11β-Hydroxysteroid dehydrogenase 1: translational and therapeutic aspects

LL Gathercole, GG Lavery, SA Morgan… - Endocrine …, 2013 - academic.oup.com
Abstract 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) interconverts the inactive
glucocorticoid cortisone and its active form cortisol. It is widely expressed and, although …

Base-Mediated Divergent Synthesis of Spiro-heterocycles Using Pronucleophiles and Ethylene via Thianthrenation

H Wu, J Wang, H **g, Z Zhang, W Ou, C Su - Organic Letters, 2024 - ACS Publications
Spirocyclic compounds are abundant in biologically active products. However, the divergent
synthesis of spirocyclic compounds using low-cost and abundant available starting materials …

Photocatalytic Deoxygenative Carboimination towards Functionalized Pyrrolines by Using Unstrained γ,δ‐Unsaturated Oximes

M Zhang, Z Zhang, Y He, T Zou, Z Qi… - Advanced Synthesis …, 2021 - Wiley Online Library
Photocatalytic deoxygenative carboimination of unstrained γ, δ‐unsaturated oximes with π‐
acceptors including trifluoromethyl alkenes, 1‐trifluoromethyl‐1, 3‐butadienes, gem …

Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)

JS Scott, FW Goldberg, AV Turnbull - Journal of Medicinal …, 2014 - ACS Publications
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) is the enzyme primarily responsible
for the regulation of intracellular cortisol levels. Inhibition of 11β-HSD1 is an attractive …

Ligand efficiency indices for an effective map** of chemico-biological space: the concept of an atlas-like representation

C Abad-Zapatero, O Perišić, J Wass, AP Bento… - Drug discovery today, 2010 - Elsevier
We propose a numerical framework that permits an effective atlas-like representation of
chemico-biological space based on a series of Cartesian planes map** the ligands with …