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Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines
- Source :
- European Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, 2015, 106, pp.15-25. ⟨10.1016/j.ejmech.2015.10.030⟩, European Journal of Medicinal Chemistry, Elsevier, 2015, 106, pp.15-25. ⟨10.1016/j.ejmech.2015.10.030⟩
- Publication Year :
- 2015
-
Abstract
- International audience; In the aim of identifying new privileged structures, we describe the 5-steps synthesis of cyclic guanidine compounds “tetrahydroisoquinoline-iminoimidazolines” derived from tetrahydroisoquinoline-hydantoin core. In order to evaluate this new minimal structure and the impact of replacing a carbonyle by a guanidine moiety, their affinity towards adenosine receptor A2A was evaluated and compared to those of tetrahydroisoquinoline-hydantoin compounds.
- Subjects :
- Models, Molecular
Receptor, Adenosine A2A
Stereochemistry
[CHIM.THER] Chemical Sciences/Medicinal Chemistry
Privileged structure
[CHIM.THER]Chemical Sciences/Medicinal Chemistry
Guanidines
A2A receptor
chemistry.chemical_compound
Structure-Activity Relationship
Tetrahydroisoquinolines
Drug Discovery
[CHIM.CRIS]Chemical Sciences/Cristallography
Moiety
Structure–activity relationship
Molecule
Humans
[CHIM.CRIS] Chemical Sciences/Cristallography
Guanidine
Imidazolines
Pharmacology
Dose-Response Relationship, Drug
Molecular Structure
[CHIM.ORGA]Chemical Sciences/Organic chemistry
Tetrahydroisoquinoline
Organic Chemistry
General Medicine
[CHIM.ORGA] Chemical Sciences/Organic chemistry
Combinatorial chemistry
Adenosine Receptor A2a
HEK293 Cells
chemistry
Purinergic P1 Receptor Antagonists
Drug Design
Iminoimidazoline
Subjects
Details
- ISSN :
- 17683254 and 02235234
- Volume :
- 106
- Database :
- OpenAIRE
- Journal :
- European journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....399a1707ea6a2583fee63e8335a93e2c