Design, Synthesis, & Anti-TB Activity of 1,3-Benzothiazinone (BTZ) Azide & Related Click Chemistry Products

University of Notre Dame Background
Tuberculosis (TB) is one of the top 10 causes of death, killing about 2 million people worldwide annually. The emergence of multi drug resistant (MDR), extensive drug resistant (XDR) and, recently, totally drug resistant strains further emphasizes the desperate, growing need for new anti-TB agents. The discovery of 1,3-benzothiazin-4-ones (BTZs), especially BTZ043, led to the identification of several other classes of nitroaromatic compounds as anti-TB agents. However, the covalent structure and the presence of a nitroso group creates limitations on BTZ043.
Technology Overview
By substituting the nitro group of the BTZ043 scaffold by an electron-withdrawing azide group (N3), researchers at University of Notre Dame have developed BTZ-azide (), a new group of anti-TB agents, with impressive inhibiting power against DprEi, an enzyme related to the cause of TB. While BTZ043 is a covalent inhibitor of DprE1, BTZ-azide is an efficient reversible and noncovalent inhibitor that provides further opportunities for development of much needed new anti-TB agents.
Further Details:
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043 doi: 10.1021/acsmedchemlett.5b00424
Stage of Development
Technology Readiness Level (TRL): 3 – Proof-of-Concept Demonstrated.

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