Design, Synthesis and Structure–Activity Relationship of Functionalized Tetrahydro‐β‐carboline Derivatives as Novel PDE5 Inhibitors
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Summary
Starting from tadalafil as a template, a series of functionalized tetrahydro‐β‐carboline derivatives have been prepared and identified as novel potent and selective PDE5 inhibitors.
- Type
- article
- Published
- 2011-03-01
- Cited by
- 23
- References
- 20
- OpenAlex
- https://openalex.org/W1967814215
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:31589673
Keywords
Chemistry, Tadalafil, Substituent, Stereochemistry, Selectivity
References
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- The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 1: 5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues.
- Tadalafil, a long-acting type 5 phosphodiesterase isoenzyme inhibitor, improves neurological functional recovery in a rat model of embolic stroke.
- Phosphodiesterase 11 (PDE11): is it a player in human testicular function?
- The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
- 13C-NMR of 1,3-Disubstituted 1,2,3,4-Tetrahydro-b-carbolines
- High biochemical selectivity of tadalafil, sildenafil and vardenafil for human phosphodiesterase 5A1 (PDE5) over PDE11A4 suggests the absence of PDE11A4 cross-reaction in patients
- A Fluorescence Polarization Assay for Cyclic Nucleotide Phosphodiesterases
- Suppression of cyclic GMP‐specific phosphodiesterase 5 promotes apoptosis and inhibits growth in HT29 cells
- Phosphodiesterase-5 inhibition augments endogenous antitumor immunity by reducing myeloid-derived suppressor cell function
- [Phosphodiesterase inhibitors: effectiveness and new applications].
- General method for the assignment of stereochemistry of 1,3-disubstituted 1,2,3,4-tetrahydro-.beta.-carbolines by carbon-13 spectroscopy
- Cyclic GMP Phosphodiesterases and Regulation of Smooth Muscle Function
- Regulation of Nitric Oxide–Sensitive Guanylyl Cyclase Cyclic GMP Phosphodiesterases and Regulation of Smooth Muscle Function Structure, Regulation, and Function of Membrane Guanylyl Cyclase Receptors, With a Focus on GC-A Cyclic GMP–Dependent Protein Kinases and the Cardiovascular System: Insights F
Cited by
- Pharmacological Importance of Optically Active Tetrahydro-β-carbolines and Synthetic Approaches to Create the C1 Stereocenter
- Exploring the PDE5 H-pocket by ensemble docking and structure-based design and synthesis of novel β-carboline derivatives
- Convenient synthesis of 1-aryl-9H-β-carboline-3-carbaldehydes and their transformation into dihydropyrimidinone derivatives by Biginelli reaction
- Novel Therapeutics: NSAIDs, Derivatives, and Phosphodiesterases
- Does phosphodiesterase 11A (PDE11A) hold promise as a future therapeutic target?
- Structure-Based Design of Novel Tetrahydro-Beta-Carboline Derivatives with a Hydrophilic Side Chain as Potential Phosphodiesterase Inhibitors
- Nickel(II)-assisted enantiomeric differentiation and quantitation of tadalafil by direct electrospray ionization mass spectrometry.
- A Role for Phosphodiesterase 11A (PDE11A) in the Formation of Social Memories and the Stabilization of Mood
- Fragmentation Pathways of Tadalafil and Its Analogues in Electrospray Ionization Tandem Mass Spectrometry
- Design, synthesis, and biological evaluation of 2‐substituted‐2,3,4,9‐tetrahydrospiro‐β‐carboline‐3‐carboxylic acid derivatives as first‐in‐class mast cell stabilizers
- Tadalafil: 15 years' journey in male erectile dysfunction and beyond
- Design, Synthesis and Structure—Activity Relationship of Functionalized Tetrahydro-β-carboline Derivatives as Novel PDE5 Inhibitors.
- A synthetic route to 1,4-disubstituted tetrahydro-β-carbolines and tetrahydropyranoindoles via ring-opening/Pictet-Spengler reaction of aziridines and epoxides with indoles/aldehydes.
- Synthesis of 1-(4-hydroxy-3-methoxyphenyl)-2,3,4,9-tetrahydro-1H-β-carboline-3-carboxylic acid derivatives as mast cell stabilizers
- Pyrrolo [3,4-b]-quinolin-9-amine compound FZU-0038-056 suppresses triple-negative breast cancer partially through inhibiting the expression of Bcl-2
- The long and winding road of designing phosphodiesterase inhibitors for the treatment of heart failure.
- Diketopiperazine-Based, Flexible Tadalafil Analogues: Synthesis, Crystal Structures and Biological Activity Profile
- NIS-promoted intramolecular cyclization of allenamides for the synthesis of tetrahydro-β-carbolines
- Isolation, bioassay and 3D-QSAR analysis of 8-isopentenyl flavonoids from Epimedium sagittatum maxim. as PDE5A inhibitors
- Advancements in Phosphodiesterase 5 Inhibitors: Unveiling Present and Future Perspectives
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