98305-60-3

Upstream product

• 1479-24-9 ethyl 2-fluorobenzoylacetate 
• 50-01-1 guanidine hydrochloride 

Downstream Products

• 74602-55-4 2-Amino-5-chloro-6-(2-fluoro-phenyl)-3H-pyrimidin-4-one 
• 74602-56-5 2-Amino-5-bromo-6-(2-fluoro-phenyl)-3H-pyrimidin-4-one 
• 74602-57-6 2-Amino-6-(2-fluoro-phenyl)-5-iodo-3H-pyrimidin-4-one 
• 423183-09-9 C₂₅H₁₈F₂N₆ 

Relevant academic research and scientific papers

Quinolinyl pyrimidines: Potent inhibitors of NDH-2 as a novel class of anti-TB agents

NDH-2 is an essential respiratory enzyme in Mycobacterium tuberculosis (Mtb), which plays an important role in the physiology of Mtb. Herein, we present a target-based effort to identify a new structural class of inhibitors for NDH-2. High-throughput screening of the AstraZeneca corporate collection resulted in the identification of quinolinyl pyrimidines as the most promising class of NDH-2 inhibitors. Structure-activity relationship studies showed improved enzyme inhibition (IC50) against the NDH-2 target, which in turn translated into cellular activity against Mtb. Thus, the compounds in this class show a good correlation between enzyme inhibition and cellular potency. Furthermore, early ADME profiling of the best compounds showed promising results and highlighted the quinolinyl pyrimidine class as a potential lead for further development.