Gabriella Guerrini
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View article: Polynitrogen Bicyclic and Tricyclic Compounds as PDE4 Inhibitors
Polynitrogen Bicyclic and Tricyclic Compounds as PDE4 Inhibitors Open
We report here two new series of designed PDE4 inhibitors, the first one showing the quinoline scaffold recently investigated by us through a fragment-based drug design strategy, and the second consisting of pyrazolo [1′,5′:1,6]pyrimido[4,…
View article: Synthesis of 3-Carboxy-6-sulfamoylquinolones and Mefloquine-Based Compounds as Panx1 Blockers: Molecular Docking, Electrophysiological and Cell Culture Studies
Synthesis of 3-Carboxy-6-sulfamoylquinolones and Mefloquine-Based Compounds as Panx1 Blockers: Molecular Docking, Electrophysiological and Cell Culture Studies Open
The membrane channel protein Panx1 is a promising therapeutic target since its involvement was demonstrated in a variety of pathologies such as neuropathic pain, ischemic stroke and cancer. As a continuation of our previous work in this fi…
View article: New heterocyclic A1/A3 adenosine receptor ligands through molecular simplification strategies
New heterocyclic A1/A3 adenosine receptor ligands through molecular simplification strategies Open
In this paper we report the synthesis of new A1/A3 adenosine receptor antagonists designed as simplification products of the A1 antagonists with pyrazolo[1′,5′:1,6]pyrimido [4,5-d]pyridazin-4(3H)-one scaffo…
View article: 3,8-Disubstituted Pyrazolo[1,5-a]quinazoline as GABAA Receptor Modulators: Synthesis, Electrophysiological Assays, and Molecular Modelling Studies
3,8-Disubstituted Pyrazolo[1,5-a]quinazoline as GABAA Receptor Modulators: Synthesis, Electrophysiological Assays, and Molecular Modelling Studies Open
As a continuation of our study in the field of GABAA receptor modulators, we report the design and synthesis of new pyrazolo[1,5-a]quinazoline (PQ) bearing at the 8-position an oxygen or nitrogen function. All the final compounds and some …
View article: Anti-Inflammatory Activity of Pyrazolo[1,5-a]quinazolines
Anti-Inflammatory Activity of Pyrazolo[1,5-a]quinazolines Open
Chronic inflammation contributes to a number of diseases. Therefore, control of the inflammatory response is an important therapeutic goal. To identify novel anti-inflammatory compounds, we synthesized and screened a library of 80 pyrazolo…
View article: Ebselen analogues with dual human neutrophil elastase (HNE) inhibitory and antiradical activity
Ebselen analogues with dual human neutrophil elastase (HNE) inhibitory and antiradical activity Open
HNE inhibitors with antiradical properties may be therapeutically beneficial for the treatment of respiratory diseases involving inflammation and oxidative stress.
View article: Ion Channels as a Therapeutic Target: Drug Design and Pharmacological Investigation
Ion Channels as a Therapeutic Target: Drug Design and Pharmacological Investigation Open
This Special Issue intends to illustrate the novelties in the field of ion channels [...]
View article: New quinoline-based PDE4 inhibitors through GSK-256066 fragment-based elaboration
New quinoline-based PDE4 inhibitors through GSK-256066 fragment-based elaboration Open
View article: 4,5-Dihydro-5-Oxo-Pyrazolo[1,5-a]Thieno[2,3-c]Pyrimidine: A Novel Scaffold Containing Thiophene Ring. Chemical Reactivity and In Silico Studies to Predict the Profile to GABAA Receptor Subtype
4,5-Dihydro-5-Oxo-Pyrazolo[1,5-a]Thieno[2,3-c]Pyrimidine: A Novel Scaffold Containing Thiophene Ring. Chemical Reactivity and In Silico Studies to Predict the Profile to GABAA Receptor Subtype Open
The isosteric replacement of the benzene with thiophene ring is a chemical modification widely applied in medicinal chemistry. Several drugs containing the thiophene ring are marketed for treating various pathologies (osteoporosis, periphe…
View article: Design, Synthesis and Pharmacological Evaluation of New Quinoline-Based Panx-1 Channel Blockers
Design, Synthesis and Pharmacological Evaluation of New Quinoline-Based Panx-1 Channel Blockers Open
Pannexins are an interesting new target in medicinal chemistry, as they are involved in many pathologies such as epilepsy, ischemic stroke, cancer and Parkinson’s disease, as well as in neuropathic pain. They are a family of membrane chann…
View article: GABAA Receptor Modulators with a Pyrazolo[1,5-a]quinazoline Core: Synthesis, Molecular Modelling Studies and Electrophysiological Assays
GABAA Receptor Modulators with a Pyrazolo[1,5-a]quinazoline Core: Synthesis, Molecular Modelling Studies and Electrophysiological Assays Open
As a continuation of our study in the GABAA receptor modulators field, we report the design and synthesis of new 8-chloropyrazolo[1,5-a]quinazoline derivatives. Molecular docking studies and the evaluation of the ‘Proximity Frequencies’ (e…
View article: CCDC 2130023: Experimental Crystal Structure Determination
CCDC 2130023: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2130022: Experimental Crystal Structure Determination
CCDC 2130022: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2045155: Experimental Crystal Structure Determination
CCDC 2045155: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: New Panx-1 Blockers: Synthesis, Biological Evaluation and Molecular Dynamic Studies
New Panx-1 Blockers: Synthesis, Biological Evaluation and Molecular Dynamic Studies Open
The channel protein Panx-1 is involved in some pathologies, such as epilepsy, ischemic stroke, cancer and Parkinson’s disease, as well as in neuropathic pain. These observations make Panx-1 an interesting biological target. We previously p…
View article: CCDC 2100699: Experimental Crystal Structure Determination
CCDC 2100699: Experimental Crystal Structure Determination Open
View article: CCDC 2100697: Experimental Crystal Structure Determination
CCDC 2100697: Experimental Crystal Structure Determination Open
View article: CCDC 2100696: Experimental Crystal Structure Determination
CCDC 2100696: Experimental Crystal Structure Determination Open
View article: CCDC 2100701: Experimental Crystal Structure Determination
CCDC 2100701: Experimental Crystal Structure Determination Open
View article: CCDC 2100698: Experimental Crystal Structure Determination
CCDC 2100698: Experimental Crystal Structure Determination Open
View article: CCDC 2100700: Experimental Crystal Structure Determination
CCDC 2100700: Experimental Crystal Structure Determination Open
View article: Nonsteroidal Anti-Inflammatory Drugs–1-Phenylethylamine Diastereomeric Salts: A Systematic Solid-State Investigation
Nonsteroidal Anti-Inflammatory Drugs–1-Phenylethylamine Diastereomeric Salts: A Systematic Solid-State Investigation Open
The solid-state investigation of the diastereomeric salts (S)-ibuprofen (S-Ibu), (S)-naproxen, (S-Nap), and (S)-ketoprofen (S-Ket) with (R)-(+)- and (S)-(-)-1-phenylethylamine, R-PEA, and S-PEA respectively, has been carried out by using a…
View article: Pyridinone Derivatives as Interesting Formyl Peptide Receptor (FPR) Agonists for the Treatment of Rheumatoid Arthritis
Pyridinone Derivatives as Interesting Formyl Peptide Receptor (FPR) Agonists for the Treatment of Rheumatoid Arthritis Open
Rheumatoid arthritis (RA) is a chronic inflammatory disease characterized by joint inflammation, cartilage damage and bone destruction. Although the pharmacological treatment of RA has evolved over the last few years, the new drugs have se…
View article: 1,5,6,7-Tetrahydro-4H-indazol-4-ones as human neutrophil elastase (HNE) inhibitors
1,5,6,7-Tetrahydro-4H-indazol-4-ones as human neutrophil elastase (HNE) inhibitors Open
View article: Synthesis, biological evaluation, molecular modeling, and structural analysis of new pyrazole and pyrazolone derivatives as N‐formyl peptide receptors agonists
Synthesis, biological evaluation, molecular modeling, and structural analysis of new pyrazole and pyrazolone derivatives as N‐formyl peptide receptors agonists Open
N‐formyl peptide receptors (FPR1, FPR2, and FPR3) play key roles in the regulation of inflammatory processes, and recently, it was demonstrated that FPR1 and FPR2 have a dual role in the progression/suppression of some cancers. Therefore, …
View article: Design and synthesis of the first indole-based blockers of Panx-1 channel
Design and synthesis of the first indole-based blockers of Panx-1 channel Open
View article: CCDC 1937512: Experimental Crystal Structure Determination
CCDC 1937512: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Exploration of nitrogen heterocycle scaffolds for the development of potent human neutrophil elastase inhibitors
Exploration of nitrogen heterocycle scaffolds for the development of potent human neutrophil elastase inhibitors Open
View article: CCDC 2012545: Experimental Crystal Structure Determination
CCDC 2012545: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Novel Sulfonamide Analogs of Sivelestat as Potent Human Neutrophil Elastase Inhibitors
Novel Sulfonamide Analogs of Sivelestat as Potent Human Neutrophil Elastase Inhibitors Open
Human neutrophil elastase (HNE) is involved in a number of essential physiological processes and has been identified as a potential therapeutic target for treating acute and chronic lung injury. Nevertheless, only one drug, Sivelestat, has…