Elsevier
European Journal of Medicinal Chemistry
,  volume 279 ,  pages 116829

Design, synthesis and antimycobacterial activity of novel benzothiazinones with improved water solubility

Xijun Zhong 1
, 
Ji-Zhou Wu 1
, 
Na Du 1
, 
Sheng Zhou 2
, 
Chao Ma 1, 3
, 
Tiezheng Xue 2
, 
Jing Li 1
, 
Jiaqi Gong 1
, 
Bin Wang 4
, 
Mingliang Liu 1
, 
Apeng Wang 1
, 
Kai Lv 1
, 
Yu Lu 4
1
 
2
 
3
 
MindRank AI Ltd., Hangzhou, 310000, China | 
4
 
Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital College of Pharmacy, Medical University, Beijing, 100149, China | 
Publication type: Journal Article
Publication date: 2024-12-01
Elsevier
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
Abstract
Nitrobenzothiazinones (BTZs) represent a novel type of antitubercular agents targeting DprE1. Two clinical candidates BTZ043 and PBTZ169, as well as many other BTZs showed potent anti-TB activity, but they are all highly lipophilic and their poor aqueous solubility is still a serious issue need to be addressed. Here, we designed and synthesized a series of new BTZ derivatives, wherein a hydrophilic COOH or NH
Found 
Found 

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GOST Copy
Zhong X. et al. Design, synthesis and antimycobacterial activity of novel benzothiazinones with improved water solubility // European Journal of Medicinal Chemistry. 2024. Vol. 279. p. 116829.
GOST all authors (up to 50) Copy
Zhong X., Wu J., Du N., Zhou S., Ma C., Xue T., Li J., Gong J., Wang B., Liu M., Wang A., Lv K., Lu Yu. Design, synthesis and antimycobacterial activity of novel benzothiazinones with improved water solubility // European Journal of Medicinal Chemistry. 2024. Vol. 279. p. 116829.
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RIS Copy
TY - JOUR
DO - 10.1016/j.ejmech.2024.116829
UR - https://linkinghub.elsevier.com/retrieve/pii/S0223523424007104
TI - Design, synthesis and antimycobacterial activity of novel benzothiazinones with improved water solubility
T2 - European Journal of Medicinal Chemistry
AU - Zhong, Xijun
AU - Wu, Ji-Zhou
AU - Du, Na
AU - Zhou, Sheng
AU - Ma, Chao
AU - Xue, Tiezheng
AU - Li, Jing
AU - Gong, Jiaqi
AU - Wang, Bin
AU - Liu, Mingliang
AU - Wang, Apeng
AU - Lv, Kai
AU - Lu, Yu
PY - 2024
DA - 2024/12/01
PB - Elsevier
SP - 116829
VL - 279
PMID - 39243457
SN - 0223-5234
SN - 1768-3254
ER -
BibTex
Cite this
BibTex (up to 50 authors) Copy
@article{2024_Zhong,
author = {Xijun Zhong and Ji-Zhou Wu and Na Du and Sheng Zhou and Chao Ma and Tiezheng Xue and Jing Li and Jiaqi Gong and Bin Wang and Mingliang Liu and Apeng Wang and Kai Lv and Yu Lu},
title = {Design, synthesis and antimycobacterial activity of novel benzothiazinones with improved water solubility},
journal = {European Journal of Medicinal Chemistry},
year = {2024},
volume = {279},
publisher = {Elsevier},
month = {dec},
url = {https://linkinghub.elsevier.com/retrieve/pii/S0223523424007104},
pages = {116829},
doi = {10.1016/j.ejmech.2024.116829}
}
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