Introduction: In the last two-three decades, antimicrobial infections have developed extreme
multiple drug-resistance and the appearance of these resistant strains is one of the biggest threats to global
health. The benzothiazole moiety is of interest to many researchers on the grounds that they constitute
a vital class of heterocyclic compounds exhibiting enormous chemotherapeutic activities. In the
drug design aspect, structure activity relationship (SAR) study is an area of exploring and continuously
refining the structural or physical properties for evoking the promising biological effects.
Methods: The present study discusses the synthesis of new antimicrobial candidates using the pharmacophore
hybrids of benzothiazole and thiophene scaffold. In an attempt to identify potential lead antimicrobial
agents, a number of N-(substituted-benzothiazol-2-yl)thiophene-2-carboxamidederivatives were
efficiently synthesized by conventional synthesis and screened in order to evaluate for their antibacterial
activity against Staphylococcus aureus (ATCC-25923) and Escherichia coli (ATCC-25922) and antifungal
activity against Aspergillus niger (ATCC- 9029) and Candida albicans (ATCC-90028) in DMF
by serial plate dilution method.
Results: Amongst the synthesized compounds, compound 3g showed significant antibacterial activity
and antifungal activity. Rest of the compounds showed moderate to less antibacterial activity against
both S. aureus and E. Coli. and antifungal activity against A. niger and C. albicans. The SAR studies
demonstrate that introducing an electron-withdrawing group at the aromatic ring has favorable effect on
the antimicrobial activity. A correlation study was also used to establish the relationship between the activity
and physicochemical parameter clogP. Titled compounds could be a promising template for future
antimicrobial drug development.
Discussion: The synthesized compounds were characterized by elemental and spectral data analysis.
Antimicrobial activity of the title compounds has been evaluated by varying the substituents in the benzothiazol