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Merck

Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.

European journal of medicinal chemistry (2011-09-13)
K D Thomas, Airody Vasudeva Adhikari, Sandeep Telkar, Imran H Chowdhury, Riaz Mahmood, Nishith K Pal, Guru Row, E Sumesh
RESUMEN

Three new series of 4-hydroxy-8-trifluoromethyl-quinoline derivatives were synthesized through multi step reactions. All the newly synthesized compounds were characterized by spectral and elemental analyses. The structure of 5j was evidenced by X-ray crystallographic study. The newly synthesized title compounds were evaluated for their antimicrobial activities including antimycobacterial activity. Amongst the tested compounds, 5b, 5e, 5h, 5j, 6c and 7c displayed promising antimicrobial activity. The mode of action of these active compounds was carried out by docking of receptor enoyl-ACP reductase with newly synthesized candidate ligands, 5b, 5e, 5h, 5j and 6c.

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Sigma-Aldrich
Ciprofloxacin, ≥98% (HPLC)
Sigma-Aldrich
Carbohydrazide, 98%
Supelco
Isoniazid, analytical standard, ≥99% (TLC)
Supelco
Ciprofloxacin, VETRANAL®, analytical standard