| dc.contributor.author | Roy, Sudeshna | en |
| dc.contributor.author | Šileikytė, Justina | en |
| dc.contributor.author | Neuenswander, Benjamin | en |
| dc.contributor.author | Hedrick, Michael P. | en |
| dc.contributor.author | Chung, Thomas D. Y. | en |
| dc.contributor.author | Aubé, Jeffrey | en |
| dc.contributor.author | Schoenen, Frank J. | en |
| dc.contributor.author | Forte, Michael A. | en |
| dc.contributor.author | Bernardi, Paolo | en |
| dc.creator | Roy, Sudeshna | en |
| dc.creator | Šileikytė, Justina | en |
| dc.creator | Neuenswander, Benjamin | en |
| dc.creator | Hedrick, Michael P. | en |
| dc.creator | Chung, Thomas D. Y. | en |
| dc.creator | Aubé, Jeffrey | en |
| dc.creator | Schoenen, Frank J. | en |
| dc.creator | Forte, Michael A. | en |
| dc.creator | Bernardi, Paolo | en |
| dc.date.accessioned | 2019-11-21T06:22:40Z | |
| dc.date.available | 2019-11-21T06:22:40Z | |
| dc.date.issued | 2015 | |
| dc.identifier.uri | http://gnosis.library.ucy.ac.cy/handle/7/56098 | |
| dc.source.uri | https://nls.ldls.org.uk/welcome.html?ark:/81055/vdc_100028748354.0x00001f | |
| dc.subject | Pharmaceutical chemistry | en |
| dc.title | N‐Phenylbenzamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore | en |
| dc.type | info:eu-repo/semantics/article | |
| dc.author.faculty | 002 Σχολή Θετικών και Εφαρμοσμένων Επιστημών / Faculty of Pure and Applied Sciences | |
| dc.author.department | Τμήμα Χημείας / Department of Chemistry | |
| dc.type.uhtype | Article | en |
| dc.description.notes | <p>ID: 1192 | en |
| dc.description.notes | In: ChemMedChem, Vol. 11, no. 3 ( 2016), p.283-288. | en |
| dc.description.notes | Summary: AbstractPersistent opening of the mitochondrial permeability transition pore (PTP), an inner membrane channel, leads to mitochondrial dysfunction and renders the PTP a therapeutic target for a host of life‐threatening diseases. Herein, we report our effort toward identifying small‐molecule inhibitors of this target through structure–activity relationship optimization studies, which led to the identification of several potent analogues around theN‐phenylbenzamide compound series identified by high‐throughput screening. In particular, compound4(3‐(benzyloxy)‐5‐chloro‐N‐(4‐(piperidin‐1‐ylmethyl)phenyl)benzamide) displayed noteworthy inhibitory activity in the mitochondrial swelling assay (EC50=280 nm), poor‐to‐very‐good physicochemical as well as in vitro pharmacokinetic properties, and conferred very high calcium retention capacity to mitochondria. From the data, we believe compound 4in this series represents a promising lead for the development of PTP inhibitors of pharmacological relevance.AbstractCalcium deregulation adjourned: Persistent opening of the mitochondrial permeability transition pore (PTP), which is a Ca2+‐release mega channel, causes cell death. Here, we describe the discovery of potentN‐phenylbenzamide compounds as PTP inhibitors that confer very high calcium retention capacity to the mitochondria that also possess good‐to‐very‐good pharmacological profiles.</p> | en |
