Put a ring on it: application of small aliphatic rings in medicinal chemistry

MR Bauer, P Di Fruscia, SCC Lucas… - RSC Medicinal …, 2021 - pubs.rsc.org
Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …

Cyclobutanes in small‐molecule drug candidates

MR van der Kolk, MACH Janssen, FPJT Rutjes… - …, 2022 - Wiley Online Library
Cyclobutanes are increasingly used in medicinal chemistry in the search for relevant
biological properties. Important characteristics of the cyclobutane ring include its unique …

Activation and signaling mechanism revealed by cannabinoid receptor-Gi complex structures

T Hua, X Li, L Wu, C Iliopoulos-Tsoutsouvas, Y Wang… - Cell, 2020 - cell.com
Human endocannabinoid systems modulate multiple physiological processes mainly
through the activation of cannabinoid receptors CB1 and CB2. Their high sequence …

Synthon-based ligand discovery in virtual libraries of over 11 billion compounds

AA Sadybekov, AV Sadybekov, Y Liu… - Nature, 2022 - nature.com
Abstract Structure-based virtual ligand screening is emerging as a key paradigm for early
drug discovery owing to the availability of high-resolution target structures,,–and ultra-large …

Crystal structures of agonist-bound human cannabinoid receptor CB1

T Hua, K Vemuri, SP Nikas, RB Laprairie, Y Wu, L Qu… - Nature, 2017 - nature.com
Abstract The cannabinoid receptor 1 (CB1) is the principal target of the psychoactive
constituent of marijuana, the partial agonist Δ9-tetrahydrocannabinol (Δ9-THC). Here we …

[HTML][HTML] A novel phytocannabinoid isolated from Cannabis sativa L. with an in vivo cannabimimetic activity higher than Δ9-tetrahydrocannabinol: Δ9 …

C Citti, P Linciano, F Russo, L Luongo, M Iannotta… - Scientific reports, 2019 - nature.com
Trans-Δ 9-tetrahydrocannabinol (Δ 9-THC) is the main compound responsible for the
intoxicant activity of Cannabis sativa L. The length of the side alkyl chain influences the …

Studies pertaining to the emerging cannabinoid hexahydrocannabinol (HHC)

DJ Nasrallah, NK Garg - ACS chemical biology, 2023 - ACS Publications
We report studies pertaining to two isomeric hexahydrocannabinols (HHCs),(9R)-HHC and
(9S)-HHC, which are derivatives of the psychoactive cannabinoids Δ9-and Δ8-THC. HHCs …

Isolation of a high-affinity cannabinoid for the human CB1 receptor from a medicinal Cannabis sativa variety: Δ9-tetrahydrocannabutol, the butyl homologue of Δ9 …

P Linciano, C Citti, L Luongo, C Belardo… - Journal of natural …, 2019 - ACS Publications
The butyl homologues of Δ9-tetrahydrocannabinol, Δ9-tetrahydrocannabutol (Δ9-THCB),
and cannabidiol, cannabidibutol (CBDB), were isolated from a medicinal Cannabis sativa …

Saturated cannabinoids: update on synthesis strategies and biological studies of these emerging cannabinoid analogs

ML Docampo-Palacios, GA Ramirez, TT Tesfatsion… - Molecules, 2023 - mdpi.com
Natural and non-natural hexahydrocannabinols (HHC) were first described in 1940 by Adam
and in late 2021 arose on the drug market in the United States and in some European …

Management of dementia-related psychosis, agitation and aggression: a review of the pharmacology and clinical effects of potential drug candidates

M Marcinkowska, J Śniecikowska, N Fajkis, P Paśko… - CNS drugs, 2020 - Springer
Along with cognitive decline, 90% of patients with dementia experience behavioral and
psychological symptoms of dementia, such as psychosis, aggression, agitation, and …