Abstract
BackgroundNitrogen containing heterocycles are widely used and investigated by pharmaceutical industry, as they are important in discovery and designing of new drug molecules. Drugs with a benzimidazole nucleus possess exclusive structural features and electron-rich atmosphere, which enable them to bind to a number of biologically important targets and result in a wide range of activities. This has served as the basis of the present study whereby new scaffolds with benzimidazole moiety were designed and synthesized.MethodsThe structures of synthesized compounds were confirmed by physicochemical and spectral means. The synthesized compounds were screened for their antimicrobial and antiproliferative activities by tube dilution and Sulforhodamine B (SRB) assays, respectively.Results and conclusionThe in vitro biological screening results revealed that compound Z24 exhibited promising antimicrobial and anticancer activities which are comparable to standards.
Highlights
The increased incidences of drug resistance caused by extensive use of antibiotics and immunosuppressive drugs have emerged as a key issue in treatment of microbial infections
It is well established that heterocyclic compounds with nitrogen and sulphur exhibit a wide scope of biological activities. 2-Mercaptobenzimidazole, for example, has been reported for their wide range of pharmacological and clinical applications [5]
The intermediate-ii on reaction with substituted aldehydes in ethanol resulted in development of title compounds (Z16–Z30) with appreciable yields
Summary
The increased incidences of drug resistance caused by extensive use of antibiotics and immunosuppressive drugs have emerged as a key issue in treatment of microbial infections. 2-chloroethanethioate (intermediate-i) was synthesized by the reaction of chloroacetyl chloride with 2-mercaptobenzimidazole, which on further reaction with corresponding anilines in presence of ethanolic solvent yielded the title compounds (Z1–Z15). The intermediate-ii on reaction with substituted aldehydes in ethanol resulted in development of title compounds (Z16–Z30) with appreciable yields.
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