Moreno-Cinos, Carlos; Sassetti, Elisa; Salado, Irene G.; Witt, Gesa; Benramdane, Siham; Reinhardt, Laura; Cruz, Cristina D.; Joossens, Jurgen; Van der Veken, Pieter; Brotz-Oesterhelt, Heike; Tammela, Paivi; Winterhalter, Mathias; Gribbon, Philip; Windshugel, Bjorn; Augustyns, Koen published the artcile< α-Amino diphenyl phosphonates as novel inhibitors of Escherichia coli ClpP protease>, Quality Control of 197638-83-8, the main research area is aminodiphenylphosphonate Escherichia ClpP protease inhibitor.
Increased Gram-neg. bacteria resistance to antibiotics is becoming a global problem, and new classes of antibiotics with novel mechanisms of action are required. The caseinolytic protease subunit P (ClpP) is a serine protease conserved among bacteria that is considered as an interesting drug target. ClpP function is involved in protein turnover and homeostasis, stress response, and virulence among other processes. The focus of this study was to identify new inhibitors of Escherichia coli ClpP and to understand their mode of action. A focused library of serine protease inhibitors based on diaryl phosphonate warheads was tested for ClpP inhibition, and a chem. exploration around the hit compounds was conducted. Altogether, 14 new potent inhibitors of E. coli ClpP were identified. Compounds 85 and 92 emerged as most interesting compounds from this study due to their potency and, resp., to its moderate but consistent antibacterial properties as well as the favorable cytotoxicity profile.
Journal of Medicinal Chemistry published new progress about Antibiotic resistance (overcoming). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Quality Control of 197638-83-8.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics