Ontology highlight
ABSTRACT:
SUBMITTER: Tseng CC
PROVIDER: S-EPMC7871173 | biostudies-literature | 2019 May
REPOSITORIES: biostudies-literature
Tseng Chih-Chung CC Baillie Gemma G Donvito Giulia G Mustafa Mohammed A MA Juola Sophie E SE Zanato Chiara C Massarenti Chiara C Dall'Angelo Sergio S Harrison William T A WTA Lichtman Aron H AH Ross Ruth A RA Zanda Matteo M Greig Iain R IR
Journal of medicinal chemistry 20190514 10
The first generation of CB<sub>1</sub> positive allosteric modulators (e.g., ZCZ011) featured a 3-nitroalkyl-2-phenyl-indole structure. Although a small number of drugs include the nitro group, it is generally not regarded as being "drug-like", and this is particularly true for aliphatic nitro groups. There are very few case studies where an appropriate bioisostere replaced a nitro group that had a direct role in binding. This may be indicative of the difficulty of replicating its binding intera ...[more]