Y
Yang Baiyuan
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Synthesis and structure-activity relationships of aryl fluorosulfate-based inhibitors as novel antitubercular agents

Abstract

To identify new compounds that can effectively inhibit Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis (TB), we screened, synthesized, and evaluated a series of novel aryl fluorosulfate derivatives for their in vitro inhibitory activity against Mtb. Compound 21b exhibited an in vitro minimum inhibitory concentration (MIC) of 0.06 mu M against Mtb, no cytotoxicity against both HEK293T and HepG2 mammalian cell lines, and had good in vivo mouse plasma exposure and lung concentration with a 20 mg/kg oral dose, which supports advanced development as a new chemical entity for TB treatment.

article Article
date_range 2024
language English
link Link of the paper
format_quote
Y
Yang Baiyuan
S
Sukheja Paridhi
Q
Qin Bo
L
Li Gencheng
B
Bare Grant
C
Cascioferro Alessandro
L
Love Melissa
P
Petrassi H.
S
Sharpless K.
M
Mcnamara Case
C
Chatterjee Arnab
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Featured Keywords
Mycobacterium tuberculosis
Aryl fluorosulfate
Sulfur (VI) fluoride exchange
Structure -activity relationship studies
Anti-TB activity
Pharmacokinetic
SuFEx
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