Synthesis and analytical characterization of new thiazol-2-(3H)-ones as human neutrophil elastase (HNE) inhibitors

Autor: Letizia Crocetti, Gianluca Bartolucci, Agostino Cilibrizzi, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Marta Menicatti, Igor A. Schepetkin, Andrei I. Khlebnikov, Mark T. Quinn, Claudia Vergelli

Publikováno v: Chemistry Central Journal, Vol 11, Iss 1, Pp 1-15 (2017)

Abstract Human neutrophil elastase (HNE) is a potent serine protease belonging to the chymotrypsin family and is involved in a variety of pathologies affecting the respiratory system. Thus, compounds able to inhibit HNE proteolytic activity could rep

Externí odkaz: https://doaj.org/article/3302c8916b934da28cb71e7bfeec8352

PSMA-targeted NIR probes for image-guided detection of prostate cancer

Autor: Agostino Cilibrizzi, Julie Tzu-Wen Wang, Siham Memdouh, Antonella Iacovone, Kate McElroy, Noor Jaffar, Jennifer Denise Young, Robert C. Hider, Philip Blower, Khuloud Al-Jamal, Vincenzo Abbate

Publikováno v: Colloids and surfaces. B, Biointerfaces. 218

Tumour-targeted near-infrared (NIR) optical imaging is an emerging tool for the detection of malignant tissues. This modality can be useful in both diagnosis and intraoperative visualisation, to help defining tumour margins and allow a more precise r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::85e32cd569d38090a94c8c5674a869f3
https://pubmed.ncbi.nlm.nih.gov/35952398

Isoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors

Autor: Letizia Crocetti, Maria Paola Giovannoni, Samuele Ciattini, Gabriella Guerrini, Giovanna Ciciani, Antonella Iacovone, Claudia Vergelli, Andrei I. Khlebnikov, Mark T. Quinn, Igor A. Schepetkin

Publikováno v: Journal of enzyme inhibition and medicinal chemistry
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 821-831 (2017)

Human neutrophil elastase (HNE) is an important target for the development of novel and selective inhibitors to treat inflammatory diseases, especially pulmonary pathologies. Here, we report the synthesis, structure–activity relationship analysis,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7bd4f4a932cfa1578c5ac35f90d07604
https://doi.org/10.1080/14756366.2017.1326915

Synthesis of Five- and Six-MemberedN-Phenylacetamido Substituted Heterocycles as Formyl Peptide Receptor Agonists

Autor: Letizia Crocetti, Antonella Iacovone, Mark T. Quinn, Richard D. Ye, Liliya N. Kirpotina, Claudia Vergelli, Gabriella Guerrini, Igor A. Schepetkin, Maria Paola Giovannoni, Giovanna Ciciani, Agostino Cilibrizzi

Publikováno v: Drug Development Research. 78:49-62

Preclinical Research Formyl peptide receptors (FPRs) are G-protein-coupled receptors that play an important role in the regulation of inflammatory process and cellular dysfunction. In humans, three different isoforms are expressed (FPR1, FPR2, and FP

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::568dc594e1b0cdc05857d9e1341e0137
https://doi.org/10.1002/ddr.21370

2-Arylacetamido-4-phenylamino-5-substituted pyridazinones as formyl peptide receptors agonists

Autor: Agostino Cilibrizzi, Claudia Vergelli, Gabriella Guerrini, Antonella Iacovone, Igor A. Schepetkin, Andrei I. Khlebnikov, Mark T. Quinn, Maria Paola Giovannoni, Richard D. Ye, Liliya N. Kirpotina, Letizia Crocetti, Giovanna Ciciani

Publikováno v: Bioorganic & Medicinal Chemistry. 24(11):2530-2543

N -Formyl peptide receptors (FPRs: FPR1, FPR2, and FPR3) are G protein-coupled receptors that play key roles in modulating immune cells. FPRs represent potentially important therapeutic targets for the development of drugs that could enhance endogeno

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0dea55da6b4d12990bbbcadc85a4dc3