Abstract

SYNTHESIS OF BENZOTHIAZOLE WITH PYRAZOLES AND STUDY ITS ANTIBACTERIAL ACTIVITY AGAINST VARIOUS MICROORGANISMS

Poonam Bhardwaj* and Arun Kumar

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Abstract

Background: Benzothiazole is a five membered thiazole ring fused to a benzene ring attached at 2nd, 3rd position having a wide range of therapeutic efficacy like antibiotic, antitubercular, anticancer, antimycotic, NSAID and antihypertensive effects. Currently, we reported synthesis of Benzothiazole derivatives by using pyrazole and screened for their antibacterial activity. Benzothiazole derivatives are found to be crucial with their great therapeutic effectiveness of in various paths of both bio-chemistry and medicinal chemistry. Pyrazole is an organic heterocyclic compound with the formula C3H3N2H. Methodology: Chemicals (Glacial Acetic Acid, Bromine, Potassium Thiocyanate, Benzene, Ethanol, Ammonia Solution, Alcohol, Ethylene Glycol) Equipments (Magnetic stirrer and Water bath) Standard drug-Streptomycin and Procaine penicillin and the bacterial activity of synthesized Benzothiazole derivative was evaluated by using Cup-plate method. Result: In present work, fluorochloroaniline was treated with Potassium thiocyanate accompanied by bromine, glacial acetic acid, NH3 to obtain 2- amino–6-fluoro-7-chloro (1,3)- benzothiozole, added in hydrazine hydrate and ethylene glycol followed by concentrated Hydrochloric Acid. It was then refluxed up to 8 hours to obtain 7-chloro-6-fluoro-2-hydrazinyl- 1,3-benzothiazole. Isolated compound was identified by the application of various related standard parameters including solubility test, TLC evaluation, laboratory interpretation findings, Infrared screening, Proton nuclear magnetic resonance and Mass spectral studies, etc. The compounds were then analyzed for their antibiotic, antitubercular, anticancer, antimycotic, NSAID and antihypertensive effects (in-vitro). Discussion: Chemical isolation and therapeutically identification of the compound 1-(7-chloro-6-fluoro-1,3-benzothiazole-2-yl)-3-methyl-1H-pyrazol-5-ol was performed for antibiotic efficacy opposed to various microbial agents and the outcome was found to be gram positive with Staphylococcus aureus and Streptococcus aureus and gram negative with respect to E.coli and pseudomonas respectively.

Keywords: Benzothiazoles, Pyrazole, Antibacterial activity, Cup-plate method, Staphylococcus aureus, E.coli, Dimethyl formamide and fluorochloroaniline.