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·2026
New Multitarget Inhibitor Potentiates Antimicrobial Activity of Aztreonam against Metallo-β-lactamase-Producing <i>Pseudomonas aeruginosa</i> Including IMP-Types
Jihyeok Kang, Dahee Lee, Mi Kyoung Kim, Joong Hoon Ahn, Tae-Won Kim, Jisun Park, Hwi Won Seo, Tae Kun Ahn, Eun Kyoung Chung, Kiho Park, Youhoon Chong
IF 6.8Journal of Medicinal Chemistry
초록

Combination of aztreonam (ATM) and avibactam (AVI) was proven to be synergistic against metallo-β-lactamase (MBL)-producing <i>Enterobacteriaceae</i>. However, in the case of <i>Pseudomonas aeruginosa</i> (PA), ATM-potentiation by AVI can hardly be achieved because PA has complex resistance mechanisms. In this study, we identified 3,7-bis-<i>O</i>-substituted difluoroquercetin derivatives <b>9</b> and <b>12</b> as new ATM-potentiating agents against the MBL-producing PAs through the simultaneous inhibition of NDM-1, OXA-10, and efflux pumps. Even though the inhibitory activity of <b>9</b> and <b>12</b> against the ATM-hydrolyzing β-lactamases (NDM-1 and OXA-10) as well as the efflux pumps is moderate, the simultaneous inhibition of multiple resistance mechanisms seems to result in remarkable potentiation of ATM against this formidable pathogen. Particularly, the IMP-producing CRPAs resistant to the most promising MBL-inhibitors were sensitized to ATM upon combination with compounds <b>9</b> and <b>12</b>. Compound <b>9</b> demonstrated potent <i>in vivo</i> rescue of ATM activity in a murine thigh infection model.

키워드
EffluxAntimicrobialAztreonamInhibitory postsynaptic potentialLead compoundBiological activityStructure–activity relationship
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article
IF / 인용수
6.8 / 0
게재 연도
2026