938-71-6Relevant academic research and scientific papers
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication
Da Costa, Laurène,Scheers, Els,Coluccia, Antonio,Casulli, Adriano,Roche, Manon,Di Giorgio, Carole,Neyts, Johan,Terme, Thierry,Cirilli, Roberto,La Regina, Giuseppe,Silvestri, Romano,Mirabelli, Carmen,Vanelle, Patrice
, p. 8402 - 8416 (2018/09/18)
Rhinoviruses (RVs) have been linked to exacerbations of many pulmonary diseases, thus increasing morbidity and/or mortality in subjects at risk. Unfortunately, the wide variety of RV genotypes constitutes a major hindrance for the development of Rhinovirus replication inhibitors. In the current investigation, we have developed a novel series of pyrazole derivatives that potently inhibit the Rhinovirus replication. Compounds 10e and 10h behave as early stage inhibitors of Rhinovirus infection with a broad-spectrum activity against RV-A and RV-B species (EC50 0.1 μM). We also evaluate the dynamics of the emerging resistance of these promising compounds and their in vitro genotoxicity. Molecular docking experiments shed light on the pharmacophoric elements interacting with residues of the drug-binding pocket.
Derivatives of 11-(1-Piperazinyl)-5H-pyrrolobenzodiazepine as Central Nervous System Agents
Wright, William B.,Greenblatt, Eugene N.,Day, Ivana P.,Quinones, Nicanor Q.,Hardy, Robert A.
, p. 462 - 465 (2007/10/02)
Four 11-(1-piperazinyl)5H-pyrrolobenzodiazepines were prepared and evaluated as central nervous system agents.All were active psychotropic agents as determined by animal screening tests.The most interesting compound, 11-(1-piperazinyl)-5H-pyrrolobenzodiazepine, showed dual activity as an antidepressant against tetrabenazine depression and as a neuroleptic as measured by protection vs. amphetamine lethality in grouped mice.
