Author: Kerstin Bystricky

0000000001040210

AUTHOR

Kerstin Bystricky

0000-0001-6717-3721

showing 8 related works from this author

A3- and A2B-fluorocorroles: synthesis, X-ray characterization and antiviral activity evaluation against human cytomegalovirus infection

2020

Twenty-nine fluorinated corroles were prepared, spectroscopically characterized, and studied for their antiviral activity against human cytomegalovirus infection. Six corroles were also fully characterized by X-ray crystallography giving insights on their geometrical features. The halogenated corroles reported herein exhibit significantly improved antiviral activity over their non-halogenated counterparts and over nitro-corrole analogs previously reported. Full activity of thirteen A3-corroles is achieved with four fluorine atoms present on the meso-phenyl ring reaching a selectivity index above 300. The maximum activity is achieved for A2B-corroles with selectivity indexes above 400. We th…

PharmacologyHuman cytomegalovirus0303 health sciences010405 organic chemistryChemistryStereochemistryOrganic ChemistryX-rayPharmaceutical Sciencechemistry.chemical_elementmedicine.diseaseRing (chemistry)01 natural sciencesBiochemistry0104 chemical sciencesCharacterization (materials science)03 medical and health sciencesDrug DiscoverymedicineFluorineMolecular MedicineMoleculeSelectivity030304 developmental biologyRSC Medicinal Chemistry

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A3- and A2B-nitrocorroles: synthesis and antiviral activity evaluation against human cytomegalovirus infection

2020

Human cytomegalovirus (hCMV) is responsible for several pathologies impacting immunocompromised patients and can trigger life-threatening infection. Several antivirals are available and are used in the clinic, but hCMV resistant strains have appeared and patients have encountered therapeutic failure. Hence, there is a constant need for new best in class or first in class antiviral molecules. We have previously shown that nitrocorroles could be used as a potent anti-hCMV agent without acute toxicity in mice. They therefore represent an excellent platform to perform structure–activity relationship (SAR) studies and to increase efficiency or reduce toxicity. We have generated original A2B- and…

PharmacologyHuman cytomegalovirus0303 health sciences010405 organic chemistrybusiness.industryOrganic ChemistryPharmaceutical Sciencemedicine.disease01 natural sciencesBiochemistryAcute toxicity0104 chemical sciences03 medical and health sciencesDrug DiscoveryToxicityCancer researchMolecular MedicineMedicineTherapeutic failurebusiness030304 developmental biologyRSC Medicinal Chemistry

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