TAXIS Pharmaceuticals Announces $2.67 Million NIH Grant to Advance Research and Development of Combination Therapy to Combat Antibiotic-Resistant Pneumonia. Originally published in NORTH BRUNSWICK, N.J., May 1, 2024 /PRNewswire-PRWeb/
FtsZ inhibitors represent a new drug class as no drugs using this mode of action (MOA) have been approved by regulators. In this paper, we present the screening and evaluation of a benzamide class that is functionalized at the alkoxy fragment targeting Gram-negative bacteria.
Efflux pumps in Gram-negative bacteria such as Pseudomonas aeruginosa provide intrinsic antimicrobial resistance by facilitating the extrusion of a wide range of antimicrobials. Approaches for combating efflux-mediated multidrug resistance involve, in part, developing indirect antimicrobial agents capable of inhibiting efflux, thus rescuing the activity of antimicrobials previously rendered inactive by efflux. Herein, TXA09155 is presented as a novel efflux pump inhibitor (EPI) formed by conformationally constraining our previously reported EPI TXA01182. TXA09155 demonstrates strong potentiation in combination with multiple antibiotics with efflux liabilities against wild-type and multidrug-resistant (MDR) P. aeruginosa.