478394-28-4

Upstream product

• 1072-98-6 5-chloro-2-pyridylamine 
• 98-09-9 benzenesulfonyl chloride 
• 182181-25-5 6-chloro-2-(chloromethyl)imidazo[1,2-a]pyridine 
• 873-55-2 sodium benzenesulfonate 
• 23886-96-6 1-chloro-3-phenylsulphonylpropane-2-one 

Downstream Products

• 478394-31-9 3-benzenesulfonyl-3-(6-chloroimidazo[1,2-a]pyridin-2-yl)-1-phenylpropan-1-ol 

Relevant academic research and scientific papers

Solid-Phase Synthesis of Imidazo[1,2-a]pyridine Using Sodium Benzenesulfinate as a Traceless Linker

(equation presented) The preparation of the first library of imidazo[1,2-a]pyridine derivatives on a solid support is described. A sulfone linker strategy was applied in the synthesis. Key steps involved in the solid-phase synthetic procedure include (i)

Targeting the human parasite Leishmania donovani: Discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series

We report herein the discovery of antileishmanial molecules based on the imidazo[1,2-a]pyridine ring. In vitro screenings of imidazopyridines belonging to our chemical library, toward the promastigotes stage of Leishmania donovani, J774A.1 murine and HepG2 human cells, permitted to identify three selective hit-compounds (12, 20 and 28). New derivatives were then synthesized to allow structure-activity and -toxicity relationships analyses, enabling to characterize a lead-compound (44) displaying both a high potency (IC 50 = 1.8 μM) and a good selectivity index, in comparison with three antileishmanial reference drug-compounds (amphotericin B, miltefosine and pentamidine). Moreover, lead-compound 44 also exhibits good in vitro activity against the intracellular amastigote stage of L. donovani. Thus, the 6-halo-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridine scaffold appears as a new promising selective antileishmanial pharmacophore, especially when substituted at position 8 by a bromine atom.