A microwave-assisted facile regioselective Fischer indole synthesis and antitubercular evaluation of novel 2-aryl-3,4-dihydro-2H-thieno[3,2-b]indoles |
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| Authors: | Subramanian Vedhanarayanan Karthikeyan Subbu Perumal Krithika Arun Shetty Perumal Yogeeswari Dharmarajan Sriram |
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| Institution: | 1. Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625 021, India;2. Medicinal Chemistry and Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science—Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Andhra Pradesh, India |
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| Abstract: | A series of novel 2-aryl-3,4-dihydro-2H-thieno3,2-b]indoles has been synthesised regioselectively in good yields from the reaction of 5-aryldihydro-3(2H)-thiophenones and arylhydrazine hydrochloride. This reaction is found to be assisted by microwaves. The thieno3,2-b]indoles were evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant M. tuberculosis (MDR-TB). Among 22 compounds screened, 2-(2,4-dichlorophenyl)-7-fluoro-3,4-dihydro-2H-thieno3,2-b]indole] (6t) was found to the most active compound with MIC of 0.4 μg/mL against MTB and MDR-TB. |
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