Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis

European Journal of Medicinal Chemistry
2020.0

Abstract

A series of 4H-chromen-4-one derivatives obtained by scaffold morphing of the benzofuran compound, TAM16, were tested for antitubercular activity. Compound 8d was active against drug-sensitive and multidrug-resistant tuberculosis. A preliminary druggability evaluation showed that compound 8d displayed favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability. An in vivo study indicated that compound 8d exhibited modest efficacy in an acute mouse model of TB after 3 weeks of treatment. Thus, 8d is a promising antituberculosis lead compound.

Knowledge Graph

Similar Paper

Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis
European Journal of Medicinal Chemistry 2020.0
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives
European Journal of Medicinal Chemistry 2010.0
Design, synthesis, and bioevaluation of a novel class of (E)-4-oxo-crotonamide derivatives as potent antituberculosis agents
Bioorganic & Medicinal Chemistry Letters 2019.0
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity
Journal of Medicinal Chemistry 2017.0
Synthesis and evaluation of in vitro antitubercular activity and antimicrobial activity of some novel 4H-chromeno[2,3-d]pyrimidine via 2-amino-4-phenyl-4H-chromene-3-carbonitriles
Medicinal Chemistry Research 2011.0
Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents
MedChemComm 2018.0
1H-Benzo[d]imidazoles and 3,4-dihydroquinazolin-4-ones: Design, synthesis and antitubercular activity
European Journal of Medicinal Chemistry 2018.0
Antitubercular properties of thiazolidin-4-ones – A review
European Journal of Medicinal Chemistry 2021.0
Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis
European Journal of Medicinal Chemistry 2022.0
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety
Bioorganic & Medicinal Chemistry Letters 2019.0