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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 (IC 50 = 179 and 120 lM) showed maximum QSI activity. Decrease in violacein production was observed in the range of 0.2-200 lM 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.

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