抗菌剂
细菌
支原体
化学
革兰氏阳性菌
生物技术
组合化学
生物
有机化学
遗传学
医学
病理
结核分枝杆菌
肺结核
作者
Christian Pinna,Piera Anna Martino,Gabriele Meroni,Valerio Massimo Sora,Lucia Tamborini,Sabrina Dallavalle,Martina Letizia Contente,Andrea Pinto
标识
DOI:10.1021/acs.jafc.1c06213
摘要
A series of vanillamides were easily synthesized, exploiting an acyltransferase from Mycobacterium smegmatis (MsAcT). After their evaluation as antimicrobial agents against a panel of Gram-positive and Gram-negative bacteria, three compounds were demonstrated to be 9-fold more effective toward Pseudomonas aeruginosa than the vanillic acid precursor. Taking into consideration the scarce permeability of the Gram-negative bacteria cell envelope when compared to Gram-positive strains or yeasts, these molecules can be considered the basis for the generation of new nature-inspired antimicrobials. To increase the process productivity and avoid any problem related to the poor water solubility of the starting material, a tailored flow biocatalyzed strategy in pure toluene was set up. While a robust immobilization protocol exploiting glyoxyl-agarose was employed to increase the stability of MsAcT, in-line work-up procedures were added downstream the process to enhance the system automation and reduce the overall costs.
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