Design, Synthesis and Biological Evaluation of Benzothiazole-thiophene Hybrids: A New Class of Potent Antimicrobial Agents

Saraswat, Pankaj and Jeyabalan, Govindasamy and Zaheen Hassan, Mohd and Jawed Ahsan, Mohammad (2017) Design, Synthesis and Biological Evaluation of Benzothiazole-thiophene Hybrids: A New Class of Potent Antimicrobial Agents. Anti-Infective Agents, 16 (1). pp. 57-63. ISSN 2211-3533

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Abstract|ملخص البحث

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 glo- bal health. The benzothiazole moiety is of interest to many researchers on the grounds that they consti- tute 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 pharma- cophore hybrids of benzothiazole and thiophene scaffold. In an attempt to identify potential lead antimi- crobial 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 anti- fungal activity against Aspergillus niger (ATCC- 9029) and Candida albicans (ATCC-90028) in DMF by serial plate dilution method. 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 ben- zothiazol moiety. 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 ac- tivity and physicochemical parameter clogP. Titled compounds could be a promising template for future antimicrobial drug development.

Item Type|تصنيف النتاج العلمي: Article| منشور علمي
Subjects | مجال موضوع النشر: Pharmaceutical Sciences
Divisions | الكلية: College of Pharmacy > Pharmacy
Depositing User: Mohd. Zaheen Hassan
Date Deposited: 04 Feb 2019 08:27
Last Modified: 04 Feb 2019 08:27

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