S. Grasso

发表

Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual screening.

A. Bitto, D. Altavilla, E. Novellino, 2016, European journal of medicinal chemistry.

Immunoproteasome‐selective and non‐selective inhibitors: A promising approach for the treatment of multiple myeloma

A. Allegra, C. Musolino, V. Innao, 2017, Pharmacology & therapeutics.

Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.

T. Schirmeister, M. D. Di Francesco, E. Nizi, 2008, Journal of medicinal chemistry.

Molecular requirement for anticonvulsant activity in a series of thiazolo-1,4-benzodiazepine derivatives and comparison with classical benzodiazepines.

A. Chimirri, M. Zappalà, S. Grasso, 1993, General pharmacology.

Development of Novel Peptidomimetics Containing a Vinyl Sulfone Moiety as Proteasome Inhibitors

T. Schirmeister, M. Zappalà, R. Ettari, 2011, ChemMedChem.

Peptide‐Based Proteasome Inhibitors in Anticancer Drug Design

M. Zappalà, R. Ettari, S. Grasso, 2014, Medicinal research reviews.

Synthesis and antitumor activity of 1,3-benzodioxole derivatives.

M. Zappalà, S. Grasso, N. Micale, 2002, Farmaco.

Convulsant effects of some xanthine derivatives in genetically epilepsy-prone rats

G. Sarro, A. Sarro, M. Zappalà, 1997, Naunyn-Schmiedeberg's Archives of Pharmacology.

7‐Chloro‐1‐(2,6‐difluorophenyl)‐1H,3H‐thiazolo[3,4‐a]benzimidazole and 1‐(2,6‐difluorophenyl)‐6‐methyl‐1H,3H‐thiazolo[3,4‐a]benzimidazole

R. Scopelliti, A. Rao, M. Zappalà, 2001 .

Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors

T. Schirmeister, S. Cosconati, M. Zappalà, 2016, Journal of enzyme inhibition and medicinal chemistry.

Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents.

T. Schirmeister, S. Cosconati, M. Zappalà, 2016, Bioorganic & medicinal chemistry letters.

Synthesis of benzothiazole derivatives and their biological evaluation as anticancer agents

A. Schimmer, M. Zappalà, S. Grasso, 2012, Medicinal Chemistry Research.

5H-[1,2,4]Oxadiazolo[5,4-d][1,5]benzothiazepines as anticonvulsant agents in DBA/2 mice

R. Gitto, A. Chimirri, G. Sarro, 1995 .

Anticonvulsant activity of pyrrolo[1',2':1,2]imidazo[4,5-b]pyridines, pyrrolo[2',1':2,3]imidazo[4,5-c] pyridines and pyrrolo[2,1-f]purines in DBA/2 mice.

G. De Sarro, A. De Sarro, A. Chimirri, 1994, General pharmacology.

Synthesis and stereochemistry of novel [1,2,4]oxadiazolo[4,5‐a][1,5]benzodiazepine derivatives

R. Ottanà, A. Chimirri, M. Zappalà, 1990 .

Thieno [3,4-b] [1,4] diazepines : synthesis and stereochemistry

R. Gitto, A. Chimirri, M. Zappalà, 1992 .

Annelated 1,5-Benzothiazepines

R. Gitto, A. Chimirri, A. Monforte, 1995 .

5H-[1,2,4]Oxadiazolo[5,4-d][1,5]benzothiazepines: Synthesis and Stereochemistry

R. Gitto, A. Chimirri, P. Monforte, 1994 .

Synthesis and structural characteristics of novel 5H-thiazolo[2,3-d][1,5]benzothiazepine derivatives

R. Scopelliti, R. Gitto, A. Chimirri, 1997 .

Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.

T. Schirmeister, S. Giofrè, M. Zappalà, 2011, European journal of medicinal chemistry.

Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.

A. Chishti, Ajay Kumar, A. Kozikowski, 2006, Journal of medicinal chemistry.

Separation of the enantiomers of anticonvulsant tricyclic pyrroloimidazolones by enantioselective HPLC. A chiral recognition model and a chiroptical study

S. Caccamese, A. Chimirri, S. Grasso, 1996 .

Pyrrolo[1',2':1,2]imidazo[4,5-b]pyridines, pyrrolo- [2',1':2,3]imidazo[4,5-c]pyridines and pyrrolo[2,1-f]purines as potential benzodiazepine ligands.

G. Genchi, A. Chimirri, P. Monforte, 1993, Farmaco.

Synthesis and in vitro anti-HIV activity of novel delta 2-1,2,4-oxadiazoline derivatives.

A. Carotti, A. Chimirri, A. Monforte, 1994, Farmaco.

Reaction of 1-formyladamantane with heterocyclic compounds. Mass spectra, antibacterial and antifungal activity

A. Chimirri, P. Monforte, S. Grasso, 1979 .

REACTION OF 1‐FORMYLADAMANTANE WITH HETEROCYCLIC COMPOUNDS. MASS SPECTRA AND ANTIBACTERIAL AND ANTIFUNGAL ACTIVITY

A. Chimirri, P. Monforte, S. Grasso, 1979 .

Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones.

M. Baraldi, G. De Sarro, A. De Sarro, 2000, Journal of medicinal chemistry.

Synthesis and Biological Activity of Novel 1H,3H-Thiazolo[3,4-a]Benzimidazoles: Non-nucleoside Human Immunodeficiency Virus Type 1 Reverse Transcriptase Inhibitors

E. De Clercq, C. Pannecouque, J. Balzarini, 1999, Antiviral chemistry & chemotherapy.

Synthesis and in vitro antitumour activity evaluation of 1-aryl-1H,3H-thiazolo[4,3-b]quinazolines.

A. Monforte, P. Monforte, M. Zappalà, 2000, European journal of medicinal chemistry.

Relationship between structure and convulsant properties of some beta-lactam antibiotics following intracerebroventricular microinjection in rats

G. De Sarro, A. De Sarro, A. Sarro, 1995, Antimicrobial agents and chemotherapy.

1-aryl-6,7-methylenedioxy-3H-quinazolin-4-ones as anticonvulsant agents.

F. Menniti, G. De Sarro, C. De Micheli, 2003, Bioorganic & medicinal chemistry letters.

Structure-activity study of 2,3-benzodiazepin-4-ones noncompetitive AMPAR antagonists: identification of the 1-(4-amino-3-methylphenyl)-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-one as neuroprotective agent.

A. Cagnotto, T. Mennini, M. Zappalà, 2008, Bioorganic & medicinal chemistry.

Ir and pmr spectra of 2-aryl-4-thiazolidinones. III. Stereochemical analysis of 2-aryl-3-(2-pyridyl)-4-thiazolidinones

M. Vigorita, A. Chimirri, S. Grasso, 1979 .

1‐Aryl‐6,7‐methylenedioxy‐3H‐quinazolin‐4‐ones as Anticonvulsant Agents.

F. Menniti, G. Sarro, M. Zappalà, 2004 .

Anti-HIV agents. V. Synthesis, structure and in vitro anti-HIV activity of novel 1H,3H-naphtho[2',3':4,5]imidazo[1,2-c]thiazoles.

R. Scopelliti, A. Chimirri, A. Rao, 1997, Farmaco.

Synthesis of benzothiazole derivatives and their biological evaluation as anticancer agents

A. Schimmer, M. Zappalà, S. Grasso, 2011, Medicinal Chemistry Research.

Synthesis of Novel 3‐(Alkylcarbamoyl)‐2‐aryl‐1,2‐dihydro‐6,7‐(methylenedioxy)‐3H‐quinazolin‐4‐ones as Anticonvulsant Agents

M. Zappalà, S. Grasso, G. Zuccalà, 2006, Chemistry & biodiversity.

GYKI 52466 and related 2,3-benzodiazepines as anticonvulsant agents in DBA/2 mice.

G. De Sarro, P. Giusti, A. De Sarro, 1995, European journal of pharmacology.

Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.

M. Leippe, T. Schirmeister, C. Gelhaus, 2010, Bioorganic & medicinal chemistry.

Synthesis, Structure and in Vitro Anti-Human Immunodeficiency virus Activity of Novel 3-Methyl-1H,3H-Thiazolo[3,4-a]Benzimidazoles

E. De Clercq, C. Pannecouque, M. Witvrouw, 1998, Antiviral chemistry & chemotherapy.

Structural Features and Anti-Human Immunodeficiency Virus (HIV) Activity of the Isomers of 1-(2′,6′-Difluorophenyl)-1H,3H-Thiazolo[3,4-a]Benzimidazole, a Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitor

E. De Clercq, J. Balzarini, M. Witvrouw, 1997 .

Anti-HIV agents. IV. Synthesis and in vitro anti-HIV activity of novel 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazoles.

R. Scopelliti, A. Chimirri, A. Monforte, 1996, Farmaco.

Anti-HIV agents II. Synthesis and in vitro anti-HIV activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles.

A. Chimirri, A. Monforte, P. Monforte, 1991, Farmaco.

Synthesis and cytotoxic activity of 1,3-benzodioxole derivatives. Note II.

M. Zappalà, S. Grasso, N. Micale, 2003, Farmaco.

Falcipain‐2 inhibitors

M. Zappalà, R. Ettari, S. Grasso, 2010, Medicinal research reviews.

Nonpeptidic Vinyl and Allyl Phosphonates as Falcipain‐2 Inhibitors

T. Schirmeister, E. Nizi, M. Zappalà, 2008, ChemMedChem.

Annelated 1,5-Benzodiazepines. Part 1. Three, Four, and Five membered Rings

R. Gitto, A. Chimirri, A. Monforte, 1993 .

Annelated 1,5-Benzodiazepines. Part II. Six Membered Rings

R. Gitto, A. Chimirri, A. Monforte, 1993 .

Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.

M. Leippe, T. Schirmeister, A. Evers, 2009, Bioorganic & medicinal chemistry.

Antimicrobial and Antiviral Activities of Some Marine Algae from Eastern Sicily

S. Caccamese, R. Azzolina, S. Grasso, 1981 .

Synthesis and Cytotoxic Activity of 1,3-Benzodioxole Derivatives. Part 2.

M. Zappalà, S. Grasso, N. Micale, 2003 .

Quinolones potentiate cefazolin-induced seizures in DBA/2 mice

G. De Sarro, A. De Sarro, A. Chimirri, 1993, Antimicrobial Agents and Chemotherapy.

Development of Rhodesain Inhibitors with a 3‐Bromoisoxazoline Warhead

T. Schirmeister, A. Pinto, L. Tamborini, 2013, ChemMedChem.

A SIMPLE AND EFFICIENT SYNTHESIS OF GYKI 52466 AND GYKI 52895

C. De Micheli, M. Zappalà, S. Grasso, 2002 .

Synthesis and anticonvulsant properties of 2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-ones.

G. De Sarro, G. Trimarchi, A. De Sarro, 1989, Journal of medicinal chemistry.

Synthesis and Molecular Modeling Studies of Derivatives of a Highly Potent Peptidomimetic Vinyl Ester as Falcipain‐2 Inhibitors

Maria Zappalà, Giovanni Grazioso, Tanja Schirmeister, 2012, ChemMedChem.

Glutamate binding-site ligands of NMDA receptors.

M. Zappalà, R. Ettari, S. Grasso, 2011, Current medicinal chemistry.

Development of Novel Selective Peptidomimetics Containing a Boronic Acid Moiety, Targeting the 20S Proteasome as Anticancer Agents

E. Novellino, A. Lavecchia, T. Schirmeister, 2014, ChemMedChem.

Anti-HIV agents. I: Synthesis and in vitro anti-HIV evaluation of novel 1H,3H-thiazolo[3,4-a]benzimidazoles.

A. Chimirri, A. Monforte, P. Monforte, 1991, Farmaco.

Synthesis and structure-activity relationships of 2,3-benzodiazepines as AMPA receptor antagonists.

C. De Micheli, M. Zappalà, S. Grasso, 2001, Mini reviews in medicinal chemistry.

Enantioseparation, absolute configuration determination, and anticonvulsant activity of (+/-)-1-(4-aminophenyl)-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-one.

G. De Sarro, P. Ficarra, M. Zappalà, 2007, Chirality.

Synthesis, chiral resolution, and enantiopharmacology of a potent 2,3-benzodiazepine derivative as noncompetitive AMPA receptor antagonist.

F. Menniti, G. De Sarro, G. Roda, 2006, Journal of medicinal chemistry.

New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists.

F. Menniti, G. De Sarro, C. De Micheli, 2006, Bioorganic & medicinal chemistry letters.

Synthesis of 2-semicarbazonomethyl-4,5-methylenedioxyphenylacetic acids as anticonvulsant agents.

F. Menniti, G. De Sarro, M. Zappalà, 2005, Farmaco.

Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.

F. Menniti, C. Costagli, A. Galli, 2003, Bioorganic & medicinal chemistry letters.

ChemInform Abstract: Synthesis and Structure-Activity Relationships of 2,3-Benzodiazepines as AMPA Receptor Antagonists.

M. Zappalà, S. Grasso, N. Micale, 2002 .

Development of novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists.

M. Zappalà, R. Ettari, S. Grasso, 2017, Bioorganic & medicinal chemistry.

Compounds with potential anti-tumor activity. VII: Synthesis and anti-tumor activity of 1-aryl-N,N'-di(1,3,4-thiadiazol-2-yl)methylenediamines

A. Chimirri, P. Monforte, M. Zappalà, 1989 .

1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.

A. Constanti, V. Libri, G. De Sarro, 1997, Journal of medicinal chemistry.

Mechanism and site of inhibition of AMPA receptors: substitution of one and two methyl groups at the 4-aminophenyl ring of 2,3-benzodiazepine and implications in the "E" site.

Congzhou Wang, R. Ettari, S. Grasso, 2015, ACS chemical neuroscience.

Mechanism of inhibition of GluA2 AMPA receptor channel opening by 2,3-benzodiazepine derivatives: functional consequences of replacing a 7,8-methylenedioxy with a 7,8-ethylenedioxy moiety.

S. Grasso, L. Niu, N. Micale, 2012, Biochemistry.

Synthesis, Chiral Resolution and Pharmacological Evaluation of a 2,3‐Benzodiazepine‐Derived Noncompetitive AMPA Receptor Antagonist

T. Mennini, P. Ficarra, M. Zappalà, 2009, ChemMedChem.

New 7,8‐Ethylenedioxy‐2,3‐benzodiazepines as Noncompetitive AMPA Receptor Antagonists.

F. Menniti, G. Sarro, M. Zappalà, 2006 .

Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists.

M. Baraldi, G. Puia, G. De Sarro, 1999, Journal of medicinal chemistry.

7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.

G. De Sarro, A. De Sarro, R. Gitto, 1998, Bioorganic & medicinal chemistry letters.

Design of 1-substituted 2-arylmethyl-4,5-methylenedioxybenzene derivatives as antiseizure agents.

G. Puia, G. De Sarro, C. De Micheli, 2004, Bioorganic & medicinal chemistry.

Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters.

G. De Sarro, L. Toma, A. De Sarro, 2002, Journal of medicinal chemistry.

Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones.

M. Baraldi, G. Puia, G. De Sarro, 2001, Bioorganic & medicinal chemistry letters.

Synthesis and anticonvulsant activity of new 2,3-benzodiazepines as AMPA receptor antagonists.

G. De Sarro, A. De Sarro, R. Gitto, 1999, Farmaco.

Aminopyrazinyl derivatives: synthesis and evaluation of antiinflammatory and related activities.

R. Ottanà, M. Vigorita, M. Zappalà, 1994, Farmaco.

Compounds with Potential Antitumor Activity. Part 7. Synthesis and Antitumor Activity of 1‐Aryl‐N,N′‐di(1,3,4‐thiadiazol‐2‐yl)methylenediamines.

A. Chimirri, A. Monforte, P. Monforte, 1989 .

Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation.

E. Novellino, Valeria La Pietra, L. Marinelli, 2015, Bioorganic & medicinal chemistry.

Synthesis and Biological Evaluation of Papain‐Family Cathepsin L‐Like Cysteine Protease Inhibitors Containing a 1,4‐Benzodiazepine Scaffold as Antiprotozoal Agents

T. Schirmeister, N. Capodicasa, A. Pinto, 2014, ChemMedChem.

Mechanism of inhibition of the GluR2 AMPA receptor channel opening by 2,3-benzodiazepine derivatives.

S. Grasso, L. Niu, N. Micale, 2008, Biochemistry.

G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.

F. Da Settimo, S. Taliani, M. Zappalà, 2016, Journal of medicinal chemistry.

Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.

E. Novellino, A. Lavecchia, T. Schirmeister, 2014, European journal of medicinal chemistry.

Identification of a new series of amides as non-covalent proteasome inhibitors.

E. Novellino, A. Lavecchia, T. Schirmeister, 2014, European journal of medicinal chemistry.

Development of peptidomimetic boronates as proteasome inhibitors.

E. Novellino, A. Lavecchia, T. Schirmeister, 2013, European journal of medicinal chemistry.

NMR conformational analysis in solution of a potent class of cysteine proteases inhibitors

A. Rotondo, M. Zappalà, R. Ettari, 2015, Structural Chemistry.

A Simple, One-Pot Synthesis of Novel 1 H , 3 H -Thiazolo-[3,4- a ]benzimidazoles

A. Chimirri, P. Monforte, M. Zappalà, 1988 .

Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.

M. Leippe, T. Schirmeister, M. D. Di Francesco, 2009, Journal of medicinal chemistry.

Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).

J. Gut, P. Rosenthal, U. Hellmich, 2017, Journal of medicinal chemistry.

Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain.

M. Leippe, T. Schirmeister, A. Evers, 2010, European journal of medicinal chemistry.

The Inhibition of Cysteine Proteases Rhodesain and TbCatB: A Valuable Approach to Treat Human African Trypanosomiasis.

L. Tamborini, M. Zappalà, R. Ettari, 2016, Mini reviews in medicinal chemistry.

NUCLEAR MAGNETIC RESONANCE AND STEREOCHEMISTRY OF VINCAMONE

A. Chimirri, P. Monforte, S. Grasso, 1983 .

Development of Novel Amides as Noncovalent Inhibitors of Immunoproteasomes

A. Bitto, E. Novellino, A. Lavecchia, 2019, ChemMedChem.

Immunoproteasome-Selective Inhibitors: A Promising Strategy to Treat Hematologic Malignancies, Autoimmune and Inflammatory Diseases.

A. Bitto, M. Zappalà, R. Ettari, 2016, Current Medicinal Chemistry.

Anti-HIV agents. III. Synthesis and in vitro anti-HIV activity of novel 1H,3H-thiazolo[3,4-a]imidazo[4,5-b]pyridines.

A. Chimirri, P. Monforte, M. Zappalà, 1994, Farmaco.

Identification of 2-thioxoimidazolidin-4-one derivatives as novel noncovalent proteasome and immunoproteasome inhibitors.

A. Bitto, R. Maccari, R. Ottanà, 2017, Bioorganic & medicinal chemistry letters.

Structure of 3‐(2‐pyridyl)‐2‐(2‐tolyl)‐1,3‐thiazolidin‐4‐one, C15H14N2OS

J. Leger, M. Vigorita, A. Chimirri, 1983 .

1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists.

A. Constanti, V. Libri, G. De Sarro, 1997, Journal of Medicinal Chemistry.

Chromatographic determination of 7,8-methylenedioxy-4H-2,3-benzodiazepin-4-ones in rat plasma: relationship to their anticonvulsant activity.

G. De Sarro, M. Zappalà, S. Grasso, 2002, Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.

Synthesis and antitumor activity evaluation of Delta2-1,2,4-oxadiazoline derivatives.

A. Chimirri, A. Rao, A. Monforte, 1996, Il Farmaco.