Scaffold Hopping in Tuberculosis Drug Discovery: Principles, Applications, and Case Studies

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F25%3A10504218" target="_blank" >RIV/00179906:_____/25:10504218 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00216208:11160/25:10504218 RIV/60162694:G44__/26:00566066

Výsledek na webu

<a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=hHGPRVtPUh" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=hHGPRVtPUh</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1021/acs.jmedchem.5c01100" target="_blank" >10.1021/acs.jmedchem.5c01100</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Scaffold Hopping in Tuberculosis Drug Discovery: Principles, Applications, and Case Studies

Popis výsledku v původním jazyce

Tuberculosis (TB) imposes a major global health challenge, aggravated by the emergence of drug-resistant Mycobacterium tuberculosis (Mtb) strains. Scaffold hopping, a medicinal chemistry approach that modifies the molecular backbone of known bioactive compounds, has emerged as a promising tool in the development of novel drugs, including TB therapeutics. This perspective provides an insight into the application of scaffold hopping across varying degrees of structural modifications, highlighting successful case studies targeting key Mtb pathways, including energy metabolism, cell wall synthesis, proteasome function, and respiratory processes. Beyond traditional and in silico methods, scaffold hopping has spurred the discovery of compounds with improved pharmacological profiles, such as improved pharmacokinetics, enhanced efficacy, reduced toxicity, and resistance circumvention. The findings support scaffold hopping&apos;s potential to address the limitations of current anti-TB drugs as a versatile and innovative approach to accelerate TB drug discovery.

Název v anglickém jazyce

Scaffold Hopping in Tuberculosis Drug Discovery: Principles, Applications, and Case Studies

Popis výsledku anglicky

Tuberculosis (TB) imposes a major global health challenge, aggravated by the emergence of drug-resistant Mycobacterium tuberculosis (Mtb) strains. Scaffold hopping, a medicinal chemistry approach that modifies the molecular backbone of known bioactive compounds, has emerged as a promising tool in the development of novel drugs, including TB therapeutics. This perspective provides an insight into the application of scaffold hopping across varying degrees of structural modifications, highlighting successful case studies targeting key Mtb pathways, including energy metabolism, cell wall synthesis, proteasome function, and respiratory processes. Beyond traditional and in silico methods, scaffold hopping has spurred the discovery of compounds with improved pharmacological profiles, such as improved pharmacokinetics, enhanced efficacy, reduced toxicity, and resistance circumvention. The findings support scaffold hopping&apos;s potential to address the limitations of current anti-TB drugs as a versatile and innovative approach to accelerate TB drug discovery.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2025

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Medicinal Chemistry

ISSN

0022-2623

e-ISSN

1520-4804

Svazek periodika

68

Číslo periodika v rámci svazku

20

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

27

Strana od-do

20903-20929

Kód UT WoS článku

001588852000001

EID výsledku v databázi Scopus

2-s2.0-105019559240