Research Articles

2018  |  Vol: 4(4)  |  Issue: 4 (July- August)  |
Synthesis of Novel Methoxy Substituted Benzothiazole Derivatives and Antibacterial Activity against Staphylococcus epidermidis

Akhilesh Gupta*

Kunwar Haribansh Singh College of Pharmacy, Jaunpur (UP), India.

*Address for Corresponding author

Akhilesh Gupta,

Kunwar Haribansh Singh College of Pharmacy, Jaunpur (U.P.), India


Objective: Staphylococcus (S.) epidermidis basically characterized as an innocuous commensal bacterium and as an important human pathogen that is responsible to one of the leading causes of infections especially on human skin. The present study was aimed to perform evaluation against infection caused by S. epidermidis for the molecules belonging benzothiazole derivatives have great importance in heterocyclic chemistry because of its potent and significant biological activities especially methoxy substitution at benzothiazole. Materials and Methods: Methoxy substituted benzothiazole derivatives were synthesized by reaction of 3-chloro-4-methoxy-aniline with potassium thiocyanate under temperature control and presence of bromine in glacial acetic acid and ammonia. Substituted nitrobenzamides then synthesized by condensation of, 2-amino-4-chloro-5-methoxy-benzothiazole with 2(3or4)-nitrobenzoylchloride acid in presence of dry pyridine and acetone. Finally, newly synthesized derivatives (K-01 to K-09) were synthesized through replacing of chlorine of nitrobenzamide by reaction with 2-nitroaniline, 3-nitroaniline, and 4-nitroaniline in presence of DMF. Analytical characterization was performed by TLC, melting point, IR and NMR spectra. Antibacterial activity was performed against S. epidermidis by cup plate method (diffusion technique) using procaine penicillin as standard. Results: Methoxy substituted benzothiazole derivatives comprising nitro group were synthesized and characterized by using analytical techniques. The synthesized derivatives screened for antibacterial activity. Compound K-03 and K-8 showed potent antibacterial activity against S. epidermidis at both concentrations 50µg/ml and 100µg/ml as compared to standard. Conclusion: Synthesis and antibacterial activity of novel methoxy substituted derivatives with nitro substitution were performed to established structure activity relation. As per the result obtain after antibacterial activity compound K-03 and K-08 showed prominent activity against S. epidermidis.

Keywords: Methoxy-benzothiazole, Benzothiazole, antibacterial, 2-substituted benzothiazole, Staphylococcus epidermidis

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