Identification of Better Pharmacokinetic Benzothiazinone Derivatives As New Antitubercular Agents

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2017 Jun 20

PMID 28626525

Citations 14

Authors

Kai Lv

Xuefu You

Bin Wang

Zengquan Wei

Yun Chai

Bo Wang

Apeng Wang

Guocheng Huang

Mingliang Liu

Yu Lu

Affiliations

Soon will be listed here.

Abstract

A series of new 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one(BTZ) derivatives containing a C-2 nitrogen spiro-heterocycle moiety based on the structures of BTZ candidates BTZ043 and PBTZ169 were designed and synthesized as new antitubercular agents. Many of them were found to have excellent activity (MIC < 0.15 μM) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistant strains. Compounds and display acceptable safety, greater aqueous solubility, and better pharmacokinetic profiles than PBTZ169, suggesting their promising potential to be lead compounds for future antitubercular drug discovery.

Citing Articles

Pharmacophore mapping, 3D QSAR, molecular docking, and ADME prediction studies of novel Benzothiazinone derivatives.

Shaikh J, Patel S, Nagani A, Shah M, Ugharatdar S, Patel A In Silico Pharmacol. 2024; 12(2):79.

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Identification of a new series of benzothiazinone derivatives with excellent antitubercular activity and improved pharmacokinetic profiles.

Xiong L, Gao C, Shi Y, Tao X, Rong J, Liu K RSC Adv. 2022; 8(20):11163-11176.

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