Ultrasound assisted,synthesis of N-(7-(R)-2-oxa-8-azabicyclo[4.2.0]octan-8-yl)isonicotinamide derivatives and their biological evaluation |
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| Authors: | Pravin Chavan Amol Salve Shivaji Jadhav Dattatraya Pansare Megha Rai |
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| Institution: | 1. Department of Chemistry, DoshiVakil College, Goregaon-Raigad, India;2. Department of Chemistry, Tarai College, Paithan, Aurangabad, India;3. Department of Chemistry, Deogiri College, Aurangabad, India;4. Department of Chemistry, Dr. Rafiq Zakaria College for Woman, Aurangabad, India |
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| Abstract: | In this study, new series of azetidine derivatives were synthesized ( 4a-n ) from isoniazide ( 1 ), Aromatic aldehydes ( 2a-n ), dihydropyran ( 3 ) using SnCl2 catalyst, via one pot multicomponent reaction/cycloaddition reaction. The synthesized azetidine derivatives were characterized by IR, 1H NMR and 13C NMR and have been screened for antimicrobial, antituberculosis and anti-inflammatory activities. In relation to Staphylococcus aureus (ATCC 25923) promising antibacterial activity was shown, compounds 4e and 4k , followed by compounds 4h , 4n , 4f , 4g and 4l . The synthesized azetidine derivatives, 4a , 4e , 4j and 4m (with zone 12 mm) displayed antituberculosis activity. But its lower potential than, the standard streptomycin (with zone 18 mm). Further 4d compound alone displayed similar activity. |
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