Synthesis, characterization and molecular docking study of novel N-substituted sulfadiazine derivatives as potential anti-mycobacterial agents

Abstract

A new series N-substituted sulfadiazine derivatives attached with different heterocyclic rings such as 4-oxo-1, 4-dihydroquinazolin[7-12], 4-oxo-2H-benzo[1,3]thiazin[13-18] have been synthesized by condensation reactions.The structures of synthesized derivatives are characterized by FT-IR, 1H-NMR, 13C-NMR spectroscopic techniques, andsome physicochemical properties. A molecular docking study is performed and the binding values show very good matchingwith experimentally result. The present work deals with newly synthesized sulfadiazine derivatives that are screened fortheir (In-vitro) antitubercular activity of compounds [7-18] is carried out against Mycobacterium tuberculosis H37Rv.compounds [8,11,13,14,15,17] are found most active (MIC=4-16 μg/mL) and compounds [7, 9,10,12,16,18] are found goodto moderately active (MIC = 62.5-125 μg/mL) by using isoniazid as standard drug.