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A novel synthesis of 2-arylbenzimidazoles in molecular sieves-MeOH system and their antitubercular activity |
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| Authors: | Amit K Chaturvedi Amit Kumar Verma Jay Prakash Thakur Sudeep Roy Shashi Bhushan Tripathi Balagani Sathish Kumar Sadiya Khwaja Naresh K Sachan Ashok Sharma Debabrata Chanda Karuna Shanker Dharmendra Saikia Arvind S Negi |
| Institution: | 1. CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow 226 015, U.P., India;2. Department of Biomedical Engineering, Faculty of Electrical Engineering and Communication, Brno University of Technology Technická 12, 61200 Brno, Czech Republic |
| Abstract: | Arylbenzimidazoles have been synthesized as antimycobacterial agents. An efficient synthesis has been developed for 2-arylbenzimidazoles from o-phenylenediamines and aromatic aldehydes in molecular sieves-methanol system. The methodology is straightforward to get 2-arylbenzimidazoles (3a–3z) in excellent yields with high chemoselectivity over 2-aryl-1-benzylbenzimidazoles (4a–4z). All these benzimidazole analogues were evaluated against M. tuberculosis in BACTEC radiometric assay. The compounds 4y and 4z exhibited potential antitubercular activity against M. tuberculosis H37RV, MIC at 16?µM and 24?µM respectively. The best compound of the series i.e. compound 4y was well tolerated by Swiss-albino mice in acute oral toxicity. Compound 4y possessing a diarylbenzimidazole core, can further be optimized for better activity. |
| Keywords: | Arylbenzimidazoles Chemoselectivity Molecular sieves Antitubercular DNA gyrase Acute oral toxicity |
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