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, and some physicochemical properties. A molecular docking study is performed and the binding values show very good matching with experimentally result. The present work deals with newly synthesized sulfadiazine derivatives that are screened for their (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 good to moderately active (MIC = 62.5-125 µg/mL) by using isoniazid as standard drug.