Nonpeptide Tachykinin Receptor Antagonists. III. SB 235375, a Low Central Nervous System-Penetrant, Potent and Selective Neurokinin-3 Receptor Antagonist, Inhibits Citric Acid-Induced Cough and Airways Hyper-reactivity in Guinea Pigs

Douglas W.P. Hay, Giuseppe Giardina, Don E. Griswold, +16

Journal of Pharmacology and Experimental Therapeutics

Discovery of a Novel Class of Selective Non-Peptide Antagonists for the Human Neurokinin-3 Receptor. 1. Identification of the 4-Quinolinecarboxamide Framework

Giuseppe Giardina, Henry M. Sarau, Carlo Farina, +8

Journal of Medicinal Chemistry

4-Quinolinecarboxamide FrameworkReceptor AntagonistsPharmacotherapyPharmaceutical ChemistryMembrane Preparation +16

Discovery of a Novel Class of Selective Non-Peptide Antagonists for the Human Neurokinin-3 Receptor. 2. Identification of (<i>S</i>)-<i>N</i>-(1-Phenylpropyl)-3-hydroxy-2- phenylquinoline-4-carboxamide (SB 223412)

Giuseppe Giardina, Luca F. Raveglia, Mario Grugni, +11

Journal of Medicinal Chemistry

Position 3Peptide SciencePharmacotherapyChemical BiologyMolecular Pharmacology +16

2-Phenyl-4-quinolinecarboxamides:  A Novel Class of Potent and Selective Non-Peptide Competitive Antagonists for the Human Neurokinin-3 Receptor

Giuseppe Giardina, Henry M. Sarau, Carlo Farina, +9

Journal of Medicinal Chemistry

Altmetric Attention ScorePeptide SciencePharmacotherapyExperimental PharmacologyPre-clinical Pharmacology +15

Stepwise Modulation of Neurokinin-3 and Neurokinin-2 Receptor Affinity and Selectivity in Quinoline Tachykinin Receptor Antagonists

Frank E. Blaney, Luca F. Raveglia, Marco Artico, +14

Journal of Medicinal Chemistry

Stepwise Chemical ModificationCompound 28PharmacotherapyMedicinal ChemistryNeurokinin-2 Receptor Affinity +17

Central and peripheral analgesic agents: chemical strategies for limiting brain penetration in kappa-opioid agonists belonging to different chemical classes.

Giuseppe Giardina, Clarke Gd, Mario Grugni, +2

PubMed

Stability of Boronic Esters to Hydrolysis: A Comparative Study

Raffaella Bernardini, Ambrogio Oliva, Alessandro Paganelli, +4

Chemistry Letters

EngineeringOrganic ChemistryAbstract Boronic EstersChemistryPharmaceutical Chemistry +14

Facile and Efficient Syntheses of Novel (S)- and (R)-3-Fluoropyrrolidines and 3,3-Difluoropyrrolidine

Giuseppe Giardina, Giulio Dondio, Mario Grugni

Synlett

Derivative (Chemistry)EngineeringChemical DerivativeFluorous SynthesisEfficient Syntheses +9

Replacement of the quinoline system in 2-phenyl-4-quinolinecarboxamide NK-3 receptor antagonists

Giuseppe Giardina, Marco Artico, Stefano Cavagnera, +14

Il Farmaco

BiochemistryFunctional SelectivityMedicineMechanism Of ActionPharmacological Agent +5

A reliable and efficient synthesis of SR 142801

Giuseppe Giardina, Mario Grugni, Roberto Rigolio, +3

Bioorganic & Medicinal Chemistry Letters

Inorganic ChemistrySr 142801Sustainable SynthesisSynthesis MethodChemistry +1