| Literature DB >> 28374540 |
Praveen Kumar V1,2, Renjitha J1,2, Fathimath Salfeena C T1,2, Ashitha K T1,2, Rangappa S Keri3, Sunil Varughese1,2, Sasidhar Balappa Somappa1,2.
Abstract
A new series of indole appended dihydronaphthalenone hybrid analogs (5a-t) have been synthesized through the Lewis acid catalyzed Michael addition of indoles to the arylidene/hetero arylidene ketones. All the synthesized derivatives are well characterized through the 1 H-NMR, 13 C-NMR, HRMS spectroscopic techniques, compound 5r was further confirmed through single crystal X-ray analysis and screened for antibacterial and antitubercular activities. Among the synthesized compounds, the minimum inhibition concentration of 5l (against Escherichia coli) and 5o & 5p (against E. coli & Staphylococcus aureus) was found to be as low as 3.12 μg/ml as compared to the standard antibacterial drug ciprofloxacin 2.5 μg/ml. In antitubercular activity, compounds 5o and 5p with minimum inhibition concentration 6.25 μg/ml were found to be comparable with that of the drugs Pyrazinamide 5 μg/ml and Streptomycin 5 μg/ml. Compounds 5i, 5j, 5m, 5n, 5q, and 5r also showed promising activity against group of organisms tested.Entities:
Keywords: Michael addition; Naphthalenones; antibiotics; antimicrobial; antitubericular; indole
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Year: 2017 PMID: 28374540 DOI: 10.1111/cbdd.12990
Source DB: PubMed Journal: Chem Biol Drug Des ISSN: 1747-0277 Impact factor: 2.817