Synthesis and Anti-TB Activity Screening of Pyrazole Conjugated Benzothiazole Analogs
Pp. 90-107 (18)
Mahesh Bhat and S.L. Belagali
Hybrid derivatives have advantage over the other compounds, because they
exhibit the enhanced bioactivity. In this chapter benzothiazole conjugated pyrazole
hybrid compounds are taken the study. Pyrazole and benzothiazole scaffolds have their
own advantage in the field of medicinal chemistry. In the present study, two series of
the pyrazole conjugated benzothiazole derivatives were synthesized by Vilsmeier-
Haack reaction, followed by the Schiff’s base formation. The newly synthesized
compounds were screened for the in-vitro and in-silico anti-TB activities. They show
moderate antibacterial and antioxidant activities. Compounds containing OH, CH3 and
Cl groups exhibit the superior antibacterial activity in the series. Majority of the
compounds exhibit the excellent in-vitro anti-TB activity, showing the MIC values up
to 1.6 μg/mL. Some compounds were show the superior activity compared to the
standard (INH and Cfx) and molecular docking studies were also carried out to know
the molecular interaction with InhA protein.
Acetophenone, Benzothiazole, Conjugation, Cyclization, Docking
score, DprE1, Hybrid molecule, Imine, InhA, In-silico, In-vitro, Isoniazid,
Molecular Docking, Phenyl hydrazine, Pyrazofurin, Pyrazole, Schiff’s Base,
Tuberculosis, Tyrosine, Vilsmeier-Haack.
Department of Chemistry, JSS College for Women, Saraswathipuram, Mysore-09, Karnataka, India.