Synthesis of C-6 Methyl Substituted Benzothiazole Derivatives and Antifungal Activity against Aspergillus Niger

Volume 1 - Issue 2

Akhilesh Gupta*

Received: June 03, 2018;   Published: June 19, 2018

DOI: 10.32474/TRSD.2018.01.000106

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Abstract

Life-threatening illness occurs due to Aspergillus species cause a spectrum of disease ranging from airway colonization. In case of respiratory tract, aspergilloma is the most common form of pulmonary involvement, which is usually accompanied by preexisting lung disease finally architectural abnormalities most commonly stem from tuberculosis, although other associated conditions, such as sarcoidosis, bronchiectasis, and neoplasm, have been documented.

Methodology: The present work comprised of synthesis and cyclization of substituted benzothiazole nucleus by reaction of substituted aniline with potassium thiocynate in presence of bromine in glacial acetic acid and ammonia under temperature control. Substituted benzothiazole then condensed with 2 (3 or 4)-nitrobenzoylchloride acid in presence of dry pyridine and acetone to get substituted nitrobenzamides. To the above product 2-nitroaniline, 3-nitroaniline, 4-nitroaniline in presence of DMF were treated to get newly synthesized derivatives (D-1 to D-09) through replacing at 7th position chlorine. Antifungal activity was performed against Aspergillus Niger by cup plate method (diffusion technique) using Griseoflavin as standard.

Result: Among, all newly synthesized derivatives compound D-5 showed potent antifungal activity against activity. Aspergillus Niger while compound D-6, D-8 and D-9 showed moderate inhibitory activity at both concentrations 50μg/ml and 100μg/ml as compared to standard.

Conclusion: In the present work efforts have been made to synthesized newer derivatives having methyl substitution at C-6 position of benzothiazole while 2-(3 or 4)-aryl-NO2 considered as rotating substitution at C-2 and C-7 position of benzothiazole nucleus to find out influence of activity due to change in substitution position against Aspergillus Niger.

Keywords Benzothiazole; Antifungal activity; 2-Substituted benzothiazole; 7-Substituted benzothiazole; Nitro benzothiazole; Cyclization of benzothiazole nucleus; Aspergillus Niger; Cup plate method (diffusion technique)

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