Abstract
Objective: The present study aims to synthesize and biological evaluation of benzimidazole derivatives as antimicrobial agents.
 Methods: 2-Methylbenzimidazole react with ethyl-chloroacetate gives N1-Ethylacetate-2-methyl-benzimidazole (1), which on reaction with thiosemicarbazide gives N1-acetylthiosemicarbazide-2-methyl-benzimidazole (2). The compound (2) on dehydrative annulation by mineral acid gives N1-(2’-amino-5’-methylene)-1’,3’,4’-thiadiazole-2-methyl-benzimidazole(3), which on condensation with various aromatic and hetero aromatic aldehydes gives N1-(2-substituted-Benzylidene-imino-5’-methylene)-1’, 3’, 4’-Thiadiazole]-2-methyl-benzimidazole(4a-4l).
 Results: The reaction sequence involves microwave-induced preparation of N1-Ethylacetate-2-methyl-benzimidazole (1) from reaction of 2-methylbenzimidazole with ethyl-chloroacetate. Further reaction with thiosemicarbazide gives N1-acetylthiosemicarbazide-2-methyl-benzimidazole (2). The compound (2) on dehydrative annulation by sulfuric acid gives N1-(2’-amino-5’-methylene)-1’,3’,4’-thiadiazole-2-methyl-benzimidazole(3), which on condensation with various aromatic and hetero aromatic aldehydes gives N1-(2-substituted-Benzylidene-imino-5’-methylene)-1’, 3’, 4’-Thiadiazole]-2-methyl-benzimidazole(4a-4l). Which were characterized by IR and 1H NMR spectral data.
 Conclusion: All the synthesized compounds were screened for antimicrobial activity by cup plate method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria.
Highlights
Benzimidazole is a heterocyclic aromatic organic compound
Benzimidazole derivatives were reported to possess analgesic and anti-inflammatory activity [1], antimicrobial [2, 3], anticancer [4], anticonvulsant [5], antiviral [6], antioxidant [7], antihypertensive [8], anti-tubercular [9], anthelmintic [10],proton pump inhibitor activity [11]. In this present study benzimidazole derivatives of Schiff bases containing various aldehydes have been synthesized. These synthesized compounds were screened for antibacterial activity by cup plate method
Melting points of all synthesized compounds were determined in open capillary tubes and were uncorrected
Summary
Benzimidazole is a heterocyclic aromatic organic compound It is an important pharmacophore and a privileged structure in medicinal chemistry. Benzimidazole derivatives were reported to possess analgesic and anti-inflammatory activity [1], antimicrobial [2, 3], anticancer [4], anticonvulsant [5], antiviral [6], antioxidant [7], antihypertensive [8], anti-tubercular [9], anthelmintic [10],proton pump inhibitor activity [11] In this present study benzimidazole derivatives of Schiff bases containing various aldehydes have been synthesized. These synthesized compounds were screened for antibacterial activity by cup plate method
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