1380733-07-2

Upstream product

• 120-80-9 benzene-1,2-diol 
• 1197-09-7 1-(3,4-dihydroxyphenyl)ethan-1-one 
• 1380732-82-0 1-(2,2-dimethylbenzo[d][1,3]dioxol-5-yl)-2-(naphthalen-2-yl-oxy)ethanone 
• 6860-95-3 1-(2,2-dimethylbenzo[d][1,3]dioxol-5-yl)ethanone 

Relevant academic research and scientific papers

Elucidation of Mycobacterium tuberculosis TypeII Dehydroquinase Inhibitors using a Fragment Elaboration Strategy

A library of novel Mycobacterium tuberculosis typeII dehydroquinase (DHQase) inhibitors were discovered through the use of a fragment elaboration approach. Putative active site binding fragments were initially assessed insilico which led to the selection of two small aromatic fragments for further investigation. Synthetic elaboration of the fragments provided a library of 34 inhibitors that exhibited low-micromolar inhibition of typeII DHQase. A number of these inhibitors also showed antibacterial activity in the low-micromolar range in screens against M. tuberculosis invitro; these now serve as lead compounds for further development of therapeutics for the treatment of tuberculosis.