864432-02-0

Upstream product

• 371-40-4 4-fluoroaniline 
• 1204-21-3 2-bromo-2',5'-dimethoxyacetophenone 
• 459-05-2 (4-fluoro-phenyl)-thiourea 
• 102-56-7 2,5-dimethoxyaniline 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 67617-97-4 N-(2,5-dimethoxyphenyl)-N'-benzoylthiocarbamide 

Relevant academic research and scientific papers

SUBSTITUTED 4-ARYLTHIAZOLES AND PROCESS OF PREPARATION THEREOF

The present invention relates to novel substituted 4-arylthiazoles, their preparation, and to their use as therapeutic agents, particularly in the prevention or treatment of tuberculosis. The resent invention articularl relates to com ounds of formula A:

Synthesis and biological evaluation of substituted 4-arylthiazol-2-amino derivatives as potent growth inhibitors of replicating Mycobacterium tuberculosis H37RV

In search of potential therapeutics for tuberculosis, we describe herein synthesis and biological evaluation of some substituted 4-arylthiazol-2-amino derivatives as modified analogues of the antiprotozoal drug Nitazoxanide (NTZ), which has recently been reported as potent inhibitor of Mtb H37Rv (Mtb MIC = 52.12 μM) with an excellent ability to evade resistance. Among the synthesized derivatives, the two compounds 7a (MIC = 15.28 μM) and 7c (MIC = 17.03 μM) have exhibited about three times better Mtb growth inhibitory activity over NTZ and are free from any cytotoxicity (Vero CC50 of 244 and 300 μM respectively). These two compounds represent promising leads for further optimization.