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Research Journal of Pharmacy and Technology
Year : 2019, Volume : 12, Issue : 10
First page : ( 4663) Last page : ( 4668)
Print ISSN : 0974-3618. Online ISSN : 0974-360X.
Article DOI : 10.5958/0974-360X.2019.00803.5

Synthesis of Novel Nitro Substituted Benzothiazole Derivatives and Antibacterial activity against Pseudomonas aeruginosa

Gupta Akhilesh*

Raigad College of Pharmacy, Mohopre (Mahad) Dist. Raigad, (Maharashtra)

*Corresponding Author E-mail: 81.akgupta@gmail.com

Online published on 24 December, 2019.

Abstract

The resistance to antimicrobial drugs is becoming an increasingly important health and economic problem, and Pseudomonas (P) aeruginosa, one of the main micro-organisms of nosocomial infections, is known for its resistance to a range of antimicrobial agents. Benzothiazole derivatives have great importance in heterocyclic chemistry because of its potent and significant biological activities especially nitro substitution at benzothiazole. Nitro substituted benzothiazole derivatives were synthesized by reaction of 3-chloro-4-nitro-aniline with potassium thiocyanate under temperature control and presence of bromine in glacial acetic acid and ammonia. Substituted benzamides then synthesized by condensation of, 2-amino-4-chloro-5-nitro-benzothiazole with 2(3or4)-benzoylchloride acid in presence of dry pyridine and acetone. Finally, newly synthesized derivatives (K01 to K-09) were synthesized through replacing of chlorine of benzamide by reaction with 2-aniline, 3-aniline, and 4-aniline in presence of DMF. Analytical characterization was performed by TLC, melting point, IR and NMR spectra. Antibacterial activity was performed against P. aeruginosa by cup plate method (diffusion technique) using procaine penicillin as standard. Nitro substituted benzothiazole derivatives comprising group were synthesized and characterized by using analytical techniques. The synthesized derivatives screened for antibacterial activity. Compound N-01, K-06 and K-08 showed potent antibacterial activity against P. aeruginosa at both concentrations 50μg/ml and 100μg/ml as compared to standard.

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Keywords

Nitro-benzothiazole, Benzothiazole, Antibacterial activity, 2-substituted benzothiazole, Cyclization of benzothiazole, Pseudomonas aeruginosa.

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