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We began analyzing https://pubs.acs.org/doi/10.1021/jm500547c, but it redirected us to https://pubs.acs.org/doi/10.1021/jm500547c. The analysis below is for the second page.
Title[redir]:
Cinnamic Anilides as New Mitochondrial Permeability Transition Pore Inhibitors Endowed with Ischemia-Reperfusion Injury Protective Effect in Vivo | Journal of Medicinal Chemistry
Description:
In this account, we report the development of a series of substituted cinnamic anilides that represents a novel class of mitochondrial permeability transition pore (mPTP) inhibitors. Initial class expansion led to the establishment of the basic structural requirements for activity and to the identification of derivatives with inhibitory potency higher than that of the standard inhibitor cyclosporine-A (CsA). These compounds can inhibit mPTP opening in response to several stimuli including calcium overload, oxidative stress, and thiol cross-linkers. The activity of the cinnamic anilide mPTP inhibitors turned out to be additive with that of CsA, suggesting for these inhibitors a molecular target different from cyclophylin-D. In vitro and in vivo data are presented for (E)-3-(4-fluoro-3-hydroxy-phenyl)-N-naphthalen-1-yl-acrylamide 22, one of the most interesting compounds in this series, able to attenuate opening of the mPTP and limit reperfusion injury in a rabbit model of acute myocardial infarction.
Title[redir]:
Cinnamic Anilides as New Mitochondrial Permeability Transition Pore Inhibitors Endowed with Ischemia-Reperfusion Injury Protective Effect in Vivo | Journal of Medicinal Chemistry
Description:
In this account, we report the development of a series of substituted cinnamic anilides that represents a novel class of mitochondrial permeability transition pore (mPTP) inhibitors. Initial class expansion led to the establishment of the basic structural requirements for activity and to the identification of derivatives with inhibitory potency higher than that of the standard inhibitor cyclosporine-A (CsA). These compounds can inhibit mPTP opening in response to several stimuli including calcium overload, oxidative stress, and thiol cross-linkers. The activity of the cinnamic anilide mPTP inhibitors turned out to be additive with that of CsA, suggesting for these inhibitors a molecular target different from cyclophylin-D. In vitro and in vivo data are presented for (E)-3-(4-fluoro-3-hydroxy-phenyl)-N-naphthalen-1-yl-acrylamide 22, one of the most interesting compounds in this series, able to attenuate opening of the mPTP and limit reperfusion injury in a rabbit model of acute myocardial infarction.
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Keywords {🔍}
mitochondrial, transition, permeability, journal, pore, molecular, acs, paolo, injury, chemistry, research, ischemiareperfusion, chen, therapeutic, cellular, medicinal, article, inhibitors, michael, access, inhibitor, pharmacological, drug, bernardi, mitochondria, cell, httpsdoiorg, andrew, information, compounds, synthesis, targets, reviews, cardioprotection, publications, calcium, oxidative, acute, myocardial, chemical, anna, pinton, wang, discovery, liu, biochemical, wei, maria, targeting, pharmacology,
Topics {✒️}
simon plyte fabio di lisa daniele fancelli marco ballarini giuseppe petrosillo 0167300 alessandra zulian spiropiperidine-based oligomycin-analog ligands vivo data vivo screening mario ordóñez mario zoratti rosa di lorenzo org/page/copyright/permissions daniele anna de grassi dietary-induced insulin resistance marco schiavone andrea ruiz‐velasco fluorescent apoptosis‐triggering molecule 3c01792 chan-jin kim f1/fo-adenosine triphosphate walter ángel trujillo-rangel miriam méndez-del villar sylvia elena totsuka-sutto real-time fluorescence measurements bax-induced cell death acs acs publications neonatal hypoxic‐ischemic encephalopathy selective directed β-arylation ischemia/reperfusion injury revisited orlando castro-e-silva mateu-armad maria virginia myocardial ischemia/reperfusion injury paolo bernardi 201500284 paolo bernardi 018 paolo bernardi 1c02912 huai-wei wang cyclophilin d-independent inhibitor n-naphthalen-1-yl-acrylamide 22 anna fantinati anna talarico 1155/2022/8624318 andrea carrer andrea carrer andrea urbani anna grassalkovich andrea rasola 1055/a-1967-2004 yang-yang shi small‐molecule inhibitors small molecule inhibitors mitochondrial permeability transition
Questions {❓}
- Mitochondrial permeability transition in cardiac ischemia–reperfusion: whether cyclophilin D is a viable target for cardioprotection?
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