3 years ago

Design, synthesis and activity evaluation study of novel substituted N -sulfonyl homoserine lactone derivatives as bacterial quorum sensing inhibitors

Junhai Xiao, Mingming Zhao, Fanhao Meng, Jingwei Liang, Qi Sun


A novel series of N-sulfonyl homoserine lactone derivatives 7a7m has been designed, synthesized, and evaluated for quorum sensing inhibitory activities through the violacein inhibition in Chromobacterium violaceum CV026. Compound 7e displayed the high level of inhibitory activity among all the compounds synthesized. Studies of structure-activity relationship indicated that compounds with thiophene group in side chain showed better activity than those substituted by furan, pyrrole, pyridyl, and phenethyl group. Thiophene substituted compounds which connected electron withdrawing group exhibited better inhibitory activity relate to those connected electron donating group. Further analysis indicated that compound bearing an electron withdrawing substituent at the position 2 of their thiophene ring exhibited superior activity against violacein production to those bearing the substituent at the position 3 and 4. Compound 7e in particular, with IC50 value of 6.19 µM, were identified as promising lead compounds for further development.

Publisher URL: https://link.springer.com/article/10.1007/s00044-017-2027-2

DOI: 10.1007/s00044-017-2027-2

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