2-Isopropylthioxanthone-Catalyzed divergent functionalization of bicyclo [1.1. 0] butanes under visible-light irradiation

PF Chen, DS Li, WT Ou, F Xue, HP Deng - Organic Letters, 2023 - ACS Publications
1, 3-Functionalized cyclobutane structural motifs are ubiquitous in natural products and
pharmaceuticals. Photoinduced alkylation of bicyclo [1.1. 0] butanes (BCBs) offers a step …

A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence

M Jiang, MCW Huizenga, JL Wirt, J Paloczi… - Nature …, 2023 - nature.com
Monoacylglycerol lipase (MAGL) regulates endocannabinoid 2-arachidonoylglycerol (2-AG)
and eicosanoid signalling. MAGL inhibition provides therapeutic opportunities but clinical …

Visible light-induced strain-release transformations of bicyclo [1.1. 0] butanes

QB Zhang, F Li, B Pan, S Zhang, XG Yue, Q Liu - Green Chemistry, 2024 - pubs.rsc.org
Bicyclo [1.1. 0] butanes, as structurally unique compounds with high strained energy and
diverse chemical properties, are becoming increasingly popular building blocks in organic …

Endocannabinoid signaling in the central nervous system

CE Martinez Ramirez, G Ruiz‐Pérez, TM Stollenwerk… - Glia, 2023 - Wiley Online Library
It is hard to overestimate the influence of the endocannabinoid signaling (ECS) system on
central nervous system (CNS) function. In the 40 years since cannabinoids were found to …

Palladium-catalyzed trans-selective synthesis of spirocyclic cyclobutanes using α, α-dialkylcrotyl-and allylhydrazones

IK Eckart-Frank, SM Wilkerson-Hill - Journal of the American …, 2023 - ACS Publications
Herein, we demonstrate the use of E/Z mixtures of α, α-disubstituted crotylhydrazones to
obtain spirocyclic vinylcyclobutanes in a diastereoselective fashion. We show 24 examples …

Cyclobutane-containing scaffolds in bioactive small molecules

C Hui, Y Liu, M Jiang, P Wu - Trends in Chemistry, 2022 - cell.com
Cyclobutane is a strained ring that is widely present in bioactive small molecules and natural
products. Contemporary advancements in the synthesis of cyclobutanes and evaluation of …

Design, synthesis, and biological evaluation of novel spirocyclic compounds as potential anti-glioblastoma agents

H Zhu, X Song, Y Pan, M Li, L Chen, P Xiao… - European Journal of …, 2023 - Elsevier
Glioblastoma (GBM) is an aggressive brain tumor with extremely limited clinical treatment
options. Because of the blood–brain barrier (BBB), it is difficult for anti-GBM drug candidates …

Structure–Activity Relationship Studies of Aryl Sulfoxides as Reversible Monoacylglycerol Lipase Inhibitors

M Jiang, MCW Huizenga, F Mohr, A Amedi… - Journal of Medicinal …, 2024 - ACS Publications
Monoacylglycerol lipase (MAGL) is the key enzyme for the hydrolysis of endocannabinoid 2-
arachidonoylglycerol (2-AG). The central role of MAGL in the metabolism of 2-AG makes it …

Structure-Guided Discovery of cis-Hexahydro-pyrido-oxazinones as Reversible, Drug-like Monoacylglycerol Lipase Inhibitors

B Kuhn, M Ritter, B Hornsperger, C Bell… - Journal of Medicinal …, 2024 - ACS Publications
Monoacylglycerol lipase (MAGL) is a key enzyme involved in the metabolism of the
endogenous signaling ligand 2-arachidonoylglycerol, a neuroprotective endocannabinoid …

Multicomponent Direct Assembly of N-Heterospirocycles Facilitated by Visible-Light-Driven Photocatalysis

OM Griffiths, SV Ley - The Journal of Organic Chemistry, 2022 - ACS Publications
N-heterospirocycles are interesting structural units found in both natural products and
medicinal compounds but have relatively few reliable methods for their synthesis. Here, we …