A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives
Article
Article Title | A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives |
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ERA Journal ID | 1566 |
Article Category | Article |
Authors | Aridoss, Gopalakrishnan, Amirthaganesan, Shanmugasundaram, Nanjundan, Nanjundan Ashok, Kim, Jong Tae, Lim, Kwon Taek, Kabilan, Senthamaraikannan and Jeong, Yeon Tae |
Journal Title | Bioorganic and Medicinal Chemistry Letters |
Journal Citation | 18 (24), pp. 6542-6548 |
Number of Pages | 7 |
Year | 2008 |
Publisher | Elsevier |
Place of Publication | United Kingdom |
ISSN | 0960-894X |
1464-3405 | |
Digital Object Identifier (DOI) | https://doi.org/10.1016/j.bmcl.2008.10.045 |
Web Address (URL) | https://www.sciencedirect.com/science/article/pii/S0960894X08012468 |
Abstract | The raise in clinical significance of multidrug-resistant bacterial pathogens has directed us to synthesize 2,6-diarylpiperidin-4-one and Δ3-tetrahydropyridin-4-ol based benzimidazole and O-arylsulfonyl derivatives. X-ray crystal structure of tetrahydropyridinol (23) confirmed a change in conformation and orientation of substituents upon amide formation. Antibacterial activities evaluated against a wide number of bacterial pathogens (both sensitive and multidrug-resistant) revealed that 19, 27 against Staphylococcus aureus, 27 against Enterococcus faecalis, and 19, 21, 23, and 27 against Enterococcus faecium are significantly good at lowest MIC90 (16 μg/mL). Inhibitory power noticed by 23 against Vancomycin–Linezolid-resistant E. faecalis and 27 against Vancomycin-resistant E. faecium are onefold better than the standard Linezolid and Trovafloxacin drugs, respectively. Moreover, antitubercular activity for the selected compounds against Mycobacterium tuberculosis H37Rv revealed that compounds 23, 24, and 27 expressed onefold improved potency compared to the standard Rifampicin drug. |
Keywords | Antibacterial activity; Tetrahydropyridine; Benzimidazole; Sulfonate; Antitubercular activity; Crystal structure |
Contains Sensitive Content | Does not contain sensitive content |
ANZSRC Field of Research 2020 | 340503. Organic chemical synthesis |
Public Notes | Files associated with this item cannot be displayed due to copyright restrictions. |
Byline Affiliations | Pukyong National University, Korea |
Annamalai University, India |
https://research.usq.edu.au/item/z22yq/a-facile-synthesis-antibacterial-and-antitubercular-studies-of-some-piperidin-4-one-and-tetrahydropyridine-derivatives
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