Singh, Shaminder ; Wanjari, Pravin J. ; Bhatia, Sonam ; Sonwane, Vijay C. ; Chakraborti, Asit K. ; Bharatam, Prasad V. (2015) Design, synthesis, biological evaluation and toxicity studies of N,N-disubstituted biguanides as quorum sensing inhibitors Medicinal Chemistry Research, 24 (5). pp. 1974-1987. ISSN 1054-2523
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Official URL: http://link.springer.com/article/10.1007%2Fs00044-...
Related URL: http://dx.doi.org/10.1007/s00044-014-1255-y
Abstract
A series of novel N,N-disubstituted biguanides (8a–8j) have been synthesized using varied secondary amines and cyanoguanidine under microwave irradiation. All the synthesized compounds were evaluated for quorum sensing inhibition (QSI) activity using Chromobacterium violaceum (ATCC12472)-based bioassay. Out of these ten compounds, two compounds 8a and 8g (IC50 = 179 and 120 µM) showed maximum QSI activity. Decrease in violacein production was observed in the range of 0.2–200 µM concentration for these respective compounds. The molecular docking studies revealed that N,N-disubstituted biguanides shared structural complementarity with CviR domain. Furthermore, TOPKAT analysis on Ames mutagenicity and carcinogenicity models had shown that this class of compounds has least probability (0.000–0.009) of exhibiting toxicity in experimental models.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Springer. |
| Keywords: | Biguanides; Microwave Assisted Synthesis; Molecular Docking; Quorum Sensing; Chromobacterium violaceum; TOPKAT Analysis |
| ID Code: | 100251 |
| Deposited On: | 20 Jan 2017 09:34 |
| Last Modified: | 20 Jan 2017 09:34 |
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