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001-es BibID:	BIBFORM118446
035-os BibID:	(cikkazonosító)217 (WoS)001152827800001 (Scopus)85186116167
Első szerző:	Bege Miklós (gyógyszerész)
Cím:	The Design, Synthesis and Mechanism of Action of Paxlovid, a Protease Inhibitor Drug Combination for the Treatment of COVID-19 / Miklós Bege, Anikó Borbás
Dátum:	2024
ISSN:	1999-4923
Megjegyzések:	The COVID-19 pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has presented an enormous challenge to health care systems and medicine. As a result of global research efforts aimed at preventing and effectively treating SARS-CoV-2 infection, vaccines with fundamentally new mechanisms of action and some small-molecule antiviral drugs targeting key proteins in the viral cycle have been developed. The most effective small-molecule drug approved to date for the treatment of COVID-19 is PaxlovidTM, which is a combination of two protease inhibitors, nirmatrelvir and ritonavir. Nirmatrelvir is a reversible covalent peptidomimetic inhibitor of the main protease (Mpro) of SARS-CoV-2, which enzyme plays a crucial role in viral reproduction. In this combination, ritonavir serves as a pharmacokinetic enhancer, it irreversibly inhibits the cytochrome CYP3A4 enzyme responsible for the rapid metabolism of nirmatrelvir, thereby increasing the half-life and bioavailability of nirmatrelvir. In this tutorial review, we summarize the development and pharmaceutical chemistry aspects of Paxlovid, covering the evolution of protease inhibitors, the warhead design, synthesis and the mechanism of action of nirmatrelvir, as well as the synthesis of ritonavir and its CYP3A4 inhibition mechanism. The efficacy of Paxlovid to novel virus mutants is also overviewed.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk viral proteases SARS-CoV-2 non-structural protein (NSP) main protease (Mpro) 3CL protease nirmatrelvir/ritonavir electrophilic warhead covalent inhibitor booster drug-drug interactions
Megjelenés:	Pharmaceutics. - 16 : 2 (2024), p. 1-17. -
További szerzők:	Borbás Anikó (1965-) (vegyész)
Pályázati támogatás:	National Laboratory of Virology, Hungary RRF-2.3.1-21-2022-00010 Egyéb
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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001-es BibID:	BIBFORM099001
035-os BibID:	(cikkazonosító)2028 (scopus)85120827765 (wos)000736524700001
Első szerző:	Le Thai, Son (gyógyszerész)
Cím:	The Very First Modification of Pleuromutilin and Lefamulin by Photoinitiated Radical Addition Reactions : synthesis and Antibacterial Studies / Thai Le Son, Páll Dávid, Rőth Erzsébet, Tran Tuyen, Debreczeni Nóra, Bege Miklós, Bereczki Ilona, Ostorházi Eszter, Milánkovits Márton, Herczegh Pál, Borbás Anikó, Csávás Magdolna
Dátum:	2021
ISSN:	1999-4923
Megjegyzések:	Pleuromutilin is a fungal diterpene natural product with antimicrobial properties, semisynthetic derivatives of which are used in veterinary and human medicine. The development of bacterial resistance to pleuromutilins is known to be very slow, which makes the tricyclic diterpene skeleton of pleuromutilin a very attractive starting structure for the development of new antibiotic derivatives that are unlikely to induce resistance. Here, we report the very first synthetic modifications of pleuromutilin and lefamulin at alkene position C19?C20, by two different photoinduced addition reactions, the radical thiol-ene coupling reaction, and the atom transfer radical additions (ATRAs) of perfluoroalkyl iodides. Pleuromutilin were modified with the addition of several alkyl- and aryl-thiols, thiol-containing amino acids and nucleoside and carbohydrate thiols, as well as perfluoroalkylated side chains. The antibacterial properties of the novel semisynthetic pleuromutilin derivatives were investigated on a panel of bacterial strains, including susceptible and multiresistant pathogens and normal flora members. We have identified some novel semisynthetic pleuromutilin and lefamulin derivatives with promising antimicrobial properties.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk pleuromutilin lefamulin synthesis photoinitiated thiol-ene addition atom transfer radical addition perfluoroalkylated side chains semisynthetic antibiotics antibacterial effect MRSA
Megjelenés:	Pharmaceutics. - 13 : 12 (2021), p. 1-21. -
További szerzők:	Páll Dávid (1998-) Rőth Erzsébet (1957-) (vegyész) Tran, Tuyen (1998-) Debreczeni Nóra (1993-) (vegyész) Bege Miklós (1991-) (gyógyszerész) Bereczki Ilona (1981-) (vegyész, antibiotikumkémikus) Ostorházi Eszter (1978-) (mikrobiológus) Milánkovits Márton (1985-) (mikrobiológus) Herczegh Pál (1947-) (vegyész, antibiotikumkémikus) Borbás Anikó (1965-) (vegyész) Csávás Magdolna (1977-) (szénhidrátkémikus, vegyész)
Pályázati támogatás:	K119509 OTKA K132870 OTKA GINOP-2.3.2-15-2016-00008 GINOP GINOP-2.3.4-15-2020-00008 GINOP
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